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4/5/18 1:43 PM CURRICULUM VITAE BRYAN L ROTH MD, PHD Selected Metrics (source): Publications: 436 (CV); Science (5); Nature (10 including 7 Articles); CELL (6) Invited Talks: 332 (CV) H Number: 107 (Publish or Perish® on March 2018) Citations: 45,000+ (Publish or Perish® on March 2018) F1000 with BL Roth as author: 40+ (F1000 search May 2017) EDUCATION 1973-1977 Carroll College (Helena, MT); BA in Biology minor in Chemistry; Maxima cum laude; Honor's Thesis: "The effects of 6-hydroxydopamine on noradrenaline levels in the cerebral cortex of neonatal mice." 1977-1983 St. Louis University School of Medicine (St.Louis, MO); MD/PhD Program in Department of Biochemistry: "Synaptic membrane and smooth microsomal opiate receptors"; PhD conferred April, 1983; MD conferred May, 1983. 1983-1984 National Naval Medical Center (Bethesda, MD); Internship in Psychiatry. 1983-1986 National Institute of Mental Health, Laboratory of Preclinical Pharmacology (Washington, DC); Erminio Costa, MD Lab Chief; Guest Worker 1988 Recombinant DNA Technology, Foundation for the Advanced Education in the Sciences, National Institute of Health, Bethesda, MD 1988-1991 Resident in Psychiatry, Stanford University Medical Center, Stanford, CA. 1989-1991 Dana Foundation Fellow in Neuroscience, Nancy Pritzker Laboratory of Molecular and Developmental Neurobiology, Stanford University School of Medicine, Stanford, CA. WORK EXPERIENCE 1984-1988 Principal Investigator, Naval Medical Research Institute (Bethesda, MD) as fulfillment of military obligation incurred during medical school (Health Professions Scholarship Program) 1987-1988 Assistant Division Head, Naval Medical Research Institute, Surgical Research Division; supervision of 1 PhD investigator, 1 PhD guest scientist, 1 MD guest scientist, 1 MD staff investigator, 1 military technician 1991-1992 Assistant Professor, Department of Psychiatry, Case Western Reserve University School of Medicine, Cleveland, OH.

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1992-2000 Associate Professor, Department of Psychiatry, Case Western Reserve University School of Medicine, Cleveland, OH. 1994-2000 Secondary appointments in Departments of Biochemistry and Neurosciences,

Case Western Reserve University School of Medicine, Cleveland, OH. 2001-present Transfer of Tenure to Department of Biochemistry with Primary Appointment in Department of Biochemistry and Secondary Appointments in Departments of Psychiatry and Neurosciences. 2003 –Promoted to Professor of Biochemistry with secondary appointment in Psychiatry effective July 1, 2003. Case Western Reserve University. 2006-present Professor of Pharmacology and Medicinal Chemistry with Tenure with secondary appointment in Psychiatry, University of North Carolina Chapel Hill Medical School. 2007-present Michael Hooker Distinguished Professor of Protein Therapeutics and Translational Proteomics, Department of Pharmacology, University of North Carolina, Chapel Hill Medical School. Joint appointment Division of Chemical Biology and Medicinal Chemistry with secondary appointment in Psychiatry. ADMINISTRATIVE EXPERIENCE CWRU Administrative Experience: 1991-1997: Coordinator for PGY-2 Didactic Seminar: Psychopharmacology, Department of Psychiatry, Case Western Reserve University Medical School. 1991-2001 Ward Psychiatrist, Schizophrenia Research Ward, Hanna Pavilion 3, University Hospitals of Cleveland, Case Western Reserve University Medical School. 1992-1994 Admissions Director, Schizophrenia Research Ward, Hanna Pavilion 3, University Hospitals of Cleveland, Case Western Reserve University Medical School. 1993-1994. Ward Director, Schizophrenia Research Ward, Hanna Pavilion 3, University Hospitals of Cleveland, Case Western Reserve University Medical School. 1993-1995 Member, VA Grant Review Committee (a Dean's Committee), Cleveland VAMC, Case Western Reserve University School of Medicine. 1994 Judge, Irwin H. Lepow Student Research Day, Feb 1, 1994; Case Western Reserve University School of Medicine. 1995 Judge, Irwin H. Lepow Student Research Day, Feb 1, 1995; Case Western Reserve University School of Medicine. 1997 Member of Search Committee for Chairman of Neurosciences Department, Case Western Reserve University School of Medicine; search culminated in appointment of Lynn

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Landmesser as Chair of Neurosciences, Case Western Reserve University Medical School. 1997-1999 Member of Research Planning Committee for the School of Medicine, Case

Western Reserve University School of Medicine. 1998-present Director, National Institute of Mental Health Psychoactive Drug Screening Program, Case Western Reserve University School of Medicine. 2003-2005 Member of Search Committee for Chairperson of Pharmacology Department, Case Western Reserve University. Search culminated in appointment of Kristof Palczewski as Chair of Pharmacology, Case Western Reserve University Medical School (2005). 2003-2004 Member of Institutional Strategic Planning Committee, Case Western Reserve University Medical School. UNC Administrative Experience 2007: UNC School of Pharmacy Recruitment Committee: led to successful recruitment of David Lawrence, PhD 2008-present: SAB Carolina Center for Integrated Chemical Biology and Drug Discovery (CICBDD; School of Pharmacy) 2009 and 2016: UNC Medical School Post-Tenure Review Committee (Basic Science) 2010-2011: UNC Medical School Accreditation Subcommittee (Research) 2010-2011: BBSP Graduate School Admissions Committee Member of several faculty search committees for pharmacology. TEACHING EXPERIENCE 1981-1983 Instructor-Medical Student Biochemistry Electives, St. Louis University School of Medicine. 1988 Lecturer in Human Biology: Psychopharmacology Stanford University. 1.5 hr lecture on "The Dopamine Hypothesis of Schizophrenia" 1988 Lecturer in Continuing Education Course: The New Neurobiology. 3 hr lecture on "AIDS and AIDS Dementia" Stanford University 1989 Lecture in Medical Psychiatry (PSY 201): "Psychiatric Aspect of AIDS"; two 1 hr lectures to first and second year medical students, Stanford University Medical School. 1989-91 Lecturer in Psychopharmacology (T206) "Biological Basis of Behavior: Psychopharmacology" 30 lecture hours each session on basic psychopharmacology to PhD students at the Pacific Graduate School of Psychology (American Psychologic Association

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Approved), Fall 1989; Winter 1989-90; Spring 1990; Summer 1990; Fall 1990; Winter 1990-91; Spring 1991. 1989 Lecturer in Human Biology: Psychopharmacology. 1.5 hr lecture on "The Dopamine Hypothesis of Schizophrenia" Stanford Univeristy (undergraduate campus). 1989 Lecturer in Psychopharmacology: "Antidepressants", 1 hr lecture for 2nd year Residents in Psychiatry, Stanford University Medical School. 1991 Lecturer in Neuropharmacology: 3 hrs on basic pharmacokinetics, antipsychotic medications and anxiolytics to Child Fellows, Stanford University School of Medicine. 1991-1998 Lectuer in Psychopharmacology: Course coordinator and lecturer; PGY-2 Residents in Psychiatry, Case Western Reserve University School of Medicine. 1991-1998 Lecturer in Psychopharmacology: Tardive Dyskinesia and Extra-Pyramidal Side-Effects; Sandoz Pharmaceutical Representatives, Case Western Reserve University School of Medicine. 1993 Lecturer in Psychiatry: Tardive Dyskinesia, Abnormal Involuntary Movements. PGY-2 Residents in Psychiatry, Case Western Reserve University School of Medicine. 1993 Lecture in Neuroscience: Role of serotonin and serotonin receptors in neuropsychiatric disorders, Basic Science for the Clinicial VI, Case Western Reserve Uiversity School of Medicine, Metro Health Medical Center (March 22, 1993). 1993 Lecturer in Pharmacology: Five 1.5 hour lectures in PHM 506 CNS Pharmacology, Department of Pharmacology, Case Western Reserve University School of Medicine. Course given to Graduate students of Pharmacology. 1993 Lecturer in Psychiatry: Serotonin. PGY-2 Residents in Psychiatry, Case Western Reserve University School of Medicine (March 31, 1993). 1994-1998 Psychopharmacology Lecture series for PGYIII Medical Students; three 1.5 hr lectures given six times/year to rotating medicals students at Hanna Pavilion. 1995 PHRM506-CNS Pharmacology; four 1.5 hour lectures to Graduate and Medical Students at CWRU. 1995, 96 PSYY3003 (Type A Elective); one 1.5 hour lecture to 2nd Year Medical Students at CWRU. 1995 Neuroscience PGY3 Didactic Seminar: one 1.5 hour lecture on serotonin. 1995 PGYI Seminar Series: one 1.5 hour lecture on schizophrenia. 1996 1 hr lecture to 2nd Year Medical Students on Antipsychotic Drugs 1996 Two 1.5 hr large group disscussions to 2nd Year Medical Students

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1996 Biochem 486: Protein structure and function. Co-course director 1997 1 hr lecture to 2nd Year Medical Students on Antipsychotic Drugs; 1 hr review session to 2nd Year Medical Students on Psychopharmacology 1997 Five 1.5 hr lectures to graduate students in PHRM 506 (CNS Pharmacology) 1997 One 1.5 hr lecture to 2nd Year Medical Students in Critical Thinking Course 1997 Examination committee for Alvin Chanko, Biochemistry 1997 One 1.5 hr lecture to 2nd Year Medical Students on Neuropharmacology

1998 Psychopharmacology Course to 2nd Year Residents

1998 Antipsychotic Drug Lecture to 1st year medical students

1998 Two 1-hr lectures to undergraduates for Biochemistry Reading Course

1999 3 hrs of lectures to Graduate students for Pharm 413 (Molecular Pharmacology)

2000 1 hr lecture to Pharm 413

2001 4 hrs lectures for Medical Student Mind Committee

2001-1hr lecture to Pharm 413

2002-Taught entire Bioc409 course (3 credit course; 36 contact hours)

2002 4 hrs lectures to Medical Student Mind committee

2003 3 hrs lectures to Medical Student Mind committee

2004 Taught entire Bioc course (3 credit course; 30 + contact hours) on Receptor Biochemistry

1996-present: served on large number of pre-thesis and thesis committees for graduate

students in Departments of Biochemistry, Pharmacology and Neurosciences, Case Western

Reserve University Medical School. Typically I serve on more than 3 committees/year of this

sort.

2005 1 hr lecture to Medical Student Mind Committee

2006 Entire course on GPCR advanced topics (Biochem Graduate Course)

UNC Teaching

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2007: 2 lectures to UNC Medical Students on Antiparkinsonian and Antipsychotic drugs.

2008: 2 lectures to UNC Medical Students on Antiparkinson and Antipsychotic drugs

2008-present 4 lectures/year to Pharmacy School Students on GPCRs and Drug Discovery

2009-present 4 lectures/year to UNC Medical Students on Antipsychotic drugs, Anti-seizure

medications, antipsychotic drugs and analgesic agents; SOM Year 2 Curriculum

2009-present PHCO 702: 4 lectures/year on CNS Pharmacology (antipsychotic drugs,

antidepressant drugs, neurological medications)

2009-2010; 2013 PHCO Grant Writing Course Co-director

Visiting Scientists/Sabbaticals

Brian Shoichet, PhD: Professor UCSF. 2011-2012 Sabbatical

H. Lee, PhD Principal Researcher, Laboratory of Functional Proteomics Korea Res. Inst. Biosci.

Biotech. Visiting scientist 2012

Joan Heller Brown, PhD. Chairman Pharmacology UCSD 2013. Sabbatical

Yusuke Goto, PhD. Sumitomo DaiNippon 2012-2014. Sponsored visiting scientist

Seiji Saito, PhD. Asubio Pharmaceuticals 2014-2016. Sponsored visiting scientist.

TRAINEES (Dates; support; most recent known position)

Eugenia Legan, MD 1984-1986; President, Healthcare Management Consulting. John Mehegan, MD 1986-1988; Assistant Professor, University of Iowa, Department of Internal Medicine. Raye Z. Litten, PhD 1984-1988; Chief, Treatment Research Branch, National Institute on Alcohol Abuse & Alcoholism (NIAAA). Joseph C. Carcillo, MD 1984-1988; Associate Professor, Critical Care Medicine and Department of Pediatrics, University of Pittsburgh School of Medicine. Salman Choudhary, PhD 1991-95; MD received and now physician.

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Esa Peka-Palvimaki, MD 1993-94; MD/PhD Student, University of Turku Medical School, Turku, Finland; Neurosurgeon, University of Helsinki and Chief Medical Officer Helsinki Hospital Margi Shah 1995; Medical Student (University of Pittsburgh). Naseem Khan, PhD 1994-1997; Visiting Research Scientist. Research Staff at Alpha Diagnostics International (San Antonio, TX) Sally Berry MD, PhD 1995-1998, Post-doctoral fellow; Formerly: Assistant Professor, Emory University Department of Psychiatry; Chief Medical Officer Tris Pharmacetuicals. Sy Fatemi MD, PhD 1993-1996; Psychiatry Resident; Professor, University of Minnesota School of Medicine, Department of Psychiatry. Laith Alsayegh 1995-1997; Undergraduate; Medical Student University of Ohio; physician Edward Hyde, PhD 1995-1997; Manager of HTS Facility, Rockefeller University, New York. (200-2004). Formerly HTS manager University of Pennsylvania, Department of Neurology; now retired. David Willins, Pharm D 1996-1999; Postdoctoral Fellow; Clinical Pharmacist, University Hospitals of Cleveland. John Gray 1996-97; Undergraduate Research Assistant; present position: MD/PhD Student Case Western Reserve University Medical School in Biochemistry; MSTP Program Fellowship and NIH Metabolism Training Program; PhD conferred 2003. Residency in Psychiatry (UCSF). Currently: Assistant Professor UC Davis Neurosciences. Wesley Kroeze, PhD: 1997-present; Associate Professor UNC Chapel Hill Medical School; NARSAD Young Investigator Award and RO1MH57635 Kurt Kristiansen, PhD: 1997-1998; Postdoctoral Fellow. Associate Professor, Department of Pharmacology, University of Tromso, Norway. Doug Sheffler, BS 1999-2005; graduate student in Biochemistry; supported by NIH NRSA; currently Assistant Professor, Burnham Institute San Diego, CA. Jason Woods, BS: 1998-2001 graduate student in Biochemistry; presently Medical Student, CWRU Medical School on medical leave David Shapiro, Ph.D.: 1998-2003; post-doctoral fellow in Biochemistry; NARSAD Young Investigator Award; CSO Bio-ID Inc. Anushree Bhatnagar, MS; 1998-2005; graduate student in Biochemistry; RO1MH61887. PhD conferred May 2005. Scientist, Hospira, Inc. Hossam Alhabachm MD; 1998-1999; post-doctoral fellow in Biochemistry. Neurologist in private practice Arizona

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Zong-Qi Xia 1999-2003: MD/PhD Student in Neurosciences; MSTP Grant and RO1MH61887; PhD conferred 2003. Residency in Neurology (Harvard). Assistant Professor Neurology, Harvard Medical School; Assistant Professor Neurology, University of Pittsburgh Medical School (present) Vincent Setola MS, 2000-2005: PhD Student in Biochemistry; American Heart Association Predoctoral Fellowship. PhD conferred May 2005; post-doctoral fellow in France (Luc Maltreaux); currently Assistant Professor, Department of Pharmacology, West Virginia University Medical School. Qi Shi, PhD 2001-2003; Postdoctoral fellow in Biochemistry and Genetics; NARSAD Young Investigator Award. Currently: Research Associate Cleveland Clinic Foundation. Laura Hong, PhD 2002-2003; supported by MH57635; Locus Pharmaceuticals, Inc. Chio-Ying Chang; 2002-2005; MS Student in Biochemistry; RO1MH57635; MS conferred May 2005. Feng Yan PhD student in Biochemistry (MS CWRU) 2004-2008; currently postdoctoral fellow UNC School of Medicine. Ryan Strachen: 2003-2010; PhD Student in Biochemistry; postdoctoral fellow Duke University (Robert Lefkowitz, HHMI); Assistant Professor UNC Medical School Department of Pharmacology. Atheir Abbas: 2004-2009 MD/PhD Student in Biochemistry; Psychiatry Resident, Columbia University Medical School; Instructor Columbia University and Fellow Department of Psychiatry. Blaine Armbruster, PhD (Pharmacology, Duke University, 2003) 2004-2007; Research Associate in Biochemistry. Supported by Individual NRSA/NIH Award. Currently, GPCR Drug Discovery, Millipore Corporation. Timothy A. Vortherms, PhD (Pharmacology, Purdue University, 2004) 2004-2007; Research Associate in Biochemistry. Supported by Department of Physiology NHLBI Training Grant. Currently: Senior Scientist, Abbvie Pharmaceutical Company. Kerry Ann (O’Conner) Grimberg, PhD (Pharmacology, Wake Forrest University, 2004); Research Associate in Biochemistry 2005-2006. Assistant Scientific Director, Case Center for Imaging Research at Case Western Reserve University Marilyn Davies RN, PhD Assistant Professor of Psychiatry—extended sabbatical in Roth lab 2003- 2006. Currently: Assistant Professor University of Pittsburgh. David Wald MD, PhD (Immunology CWRU); Postdoctoral fellow 2003-2006; Assistant Professor Department of Pathology, Case Western Reserve University. Tabitha Bonnaci, PhD (Pharmacology, University of Rochester School of Medicine; 2005); Research Associate in Biochemistry 2006. Manager, Regulatory Affairs-CMC at Amgen

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Ying Pei, PhD (Pharmacology, University of Connecticut). Research Associate in Phamacology 2007-08. Prem Yadav, PhD (Pharmacology, University of Madras). Research Associate in Phamacology 2007-2011. Currently Senior Scientist, CDRI, Lucknow, India. X-P Huang, PhD (Pharmacology, University of Toledo) Research Associate in Phamacology 2007-2013. Assistant Professor UNC Pharmacology 2014- John Allen, PhD (Pharmacology, University of Illinois, Chicago) Research Associate in Phamacology 2007-2011. Principal Scientist, Pfizer Pharmaceuticals (2011-2016); Assistant Professor University of Texas Medical Branch, Department of Pharmacology. Samarpan Majunder, PhD Senior Research Associate in Phamacology 2006-2009; Sarah Rogan MD/PhD student in Pharmacology (BS Wesleyen University) 2007-2010. Currently Resident in OB/Gyn. Joe Rittner PhD student in Medicinal Chemistry (BS North Carolina State University) 2006-2008 (left graduate school because of medical reasons). Currently postdoctoral fellow Duke University. Daniel Urban PhD student in Pharmacology, 2008-2013; pending appointment as staff scientist NCATS/NIH Marty Farrell, PhD student in Pharmacology, 2008-2013; currently post-doctoral fellow Patrick Sullivan Lab UNC. Shuyun Dong, MD, PhD—postdoctoral fellow in Pharmacology (PhD University of Massachusetts) 2008-2010; currently Research Assistant Professor University of Utah Pharmaceutics and Pharmaceutical Chemistry HM Lee, PhD—postdoctoral fellow in Pharmacology (PhD University of Southern Florida); 2011-2015 Hu Zhu, PhD—postdoctoral fellow in Pharmacology; 2010-present Eyal Vardy,PhD—postdoctoral fellow in Pharmacology; 2010-2014; currently Senior Scientist, Merck. Kate White, graduate student in pharmacology 2011-2014; currently postdoctoral fellow Ray Stevens Lab (Scripps). John McCorvey, PhD—postdoctoral fellow in pharmacology (Purdue University) 2012-2018; Assistant Professor of Cell Biology, Medical College of Wisconsin (start date July 2018) Patrick Guiguire, PhD –research associate /postdoctoral fellow (Canada PhD) 2012-2015; Assistant Professor University of Ottawa (July 2015)

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Daniel Wacker, PhD—postdoctoral fellow in pharmacology (Scripps) 2014-2018; Assistant Professor Pharmacology and Chemical Biology, Mt Sinai School of Medicine. Justin English, PhD-postdoctoral fellow in pharmacology (UNC) 2014- Shen Wang, PhD—postdoctoral fellow in pharmacology (Shanghai Institute of Biochemistry and Cell Biology) 2014- Brian Krumm, PhD—postdoctoral fellow in pharmacolgogy ; 2016- Kate Lansu, graduate student in Pharmacology (2014-2017); NIH Training Grant (2015-16); PhRMA Foundation Predoctoral Awardee (2016-2017). Postdoctoral Fellow Yale University Tao Che, PhD—postdoctoral fellow in pharmacology; PhD Case Western Reserve University Biochemistry; 2015- Zach Schools, graduate student in Pharmacology (2015-); NIH Training Grant (2016-) Reid Olson, graduate student in Pharmacology (2016-); NIMH Individual NRSA CONSULTATIONS Berlex Pharmaceuticals-1987 Marion Merrill Dow-1991-1993 SK Corporaration 1997-present; Member Scientific Advisory Board 1998-present Otsuka International 1998-2000; 2001-present Bristol Myers Squibb 2001-present Neotherapeutics 2002 Arena Pharmaceuticals 2002-2005 Forest Pharmaceuticals; Member of Psychiatric Advisory Board 2002 Eli Lilly 2002 Pfizer 2003; Member of Cardiovascular Safety Advisory Board Memory Pharmaceuticals, 2004 Sumitomo Pharmaceuticals, 2004 Johnson and Johnson/Janssen Pharmaceuticals, 2005- Abbott Labs, 2005 Astra Zenica Pharmaceuticals, 2005 AryX Pharmaceuticals, 2006- GlaxoSmithKline, 2006- AMRI, Inc Supernus Pharmaceuticals 2007-2008 Epix Pharmacueticals 2006-2007 Merck 2008; 2010; 2014 Wyeth 2007 Wyeth/Solvay Alliance 2007 DaiNippon Sumitomo 2007 Invitrogen 2008-2010

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LaboPharma 2007 Mediavation 2007-2009 Galenea Pharmaceuticals 2009 Nereus Pharmaceuticals 2010 Venrock Investments 2010 Pfizer Scientific Advisory Board CNS 2012-2016 RuiYi Pharmaceuticals 2013-2014 Merck 2014 Novartis 2014 Roche 2015 PATENTS AND INVENTIONS (partial listing; many others published or submitted) PATENTS (US ISSUED PATENTS IN BOLD) AND PATENT APPLICATIONS (MOST RECENT LISTED FIRST) Licensed patents: BTG International (#’s: 17, 24-26, 31-39); Galenea Pharmaceuticals (13, 16, 18-20, 22, 27, 29, 30) 1. US 20140243333 SYNTHESIS OF FUNCTIONALIZED OCTAHYDRO-ISOQUINOLIN-1-ONE-8-CARBOXYLIC ESTERS AND ANALOGS, AND THERAPEUTIC METHODS Jeffrey Aube, Bryan L. Roth, Partha Ghosh, Kevin J. Frankowski. Publication date: 2014-08-28 2. US 8754132 Highly selective 5-HT(2C) receptor agonists that show anti-psychotic effects with antagonist activity at the 5-HT(2B) receptor. Alan Kozikowski, Bryan Roth, Andreas Svennebring, Sung Jin Cho. Publication date: 2013-05-06 3. US 8735391 Synthesis of functionalized octahydro-isoquinolin-1-one-8-carboxamides, octahydro-isoquinolin-1-one-8-carboxylic esters and analogs, and therapeutic methods Jeffrey Aube, Bryan L. Roth, Partha Ghosh, Kevin J. Frankowski. Publication date: 2009-09-25 4. US 20130317018 A1 Methods and Compositions for Unsilencing Imprinted Genes. Benjamin David Philpot, Mark John Zylka, Bryan Leo Roth, John Arthur Allen, Hsien-Sung Huang, Publication date: 2013-11-28 5. US 8492591 Highly selective 5-HT(2C) receptor agonists that show anti-psychotic effects with antagonist activity at the 5-HT(2B) receptor. Alan Kozikowski, Bryan Roth, Andreas Svennebring, Sung Jin Cho, Publication date: 2011-02-03 6. US 9,156,822 Functionally Selective Ligands of Dopamine D2 Receptors. Jian Jin, Bryan Roth, Stephen Frye, Publication date: 2015-10-13 7. EP 2531485 A2 HIGHLY SELECTIVE 5-HT(2C) RECEPTOR AGONISTS HAVING ANTAGONIST ACTIVITY AT THE 5-HT(2B) RECEPTOR, Alan Kozikowski, Bryan Roth, Andreas Svennebring, Gang Chen, CHO, Sung, Jin, Publication date: 2011-02-03

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8. AU 2011212930 A1 Highly selective 5-HT(2C) receptor agonists having antagonist activity at the 5-HT(2B) receptor, Alan Kozikowski, Bryan Roth, Andreas Svennebring, Gang Chen, Sung Jin Cho, Publication date: 2011-02-03 9. WO 2012003418 A2 FUNCTIONALLY SELECTIVE LIGANDS OF DOPAMINE D2 RECEPTORS. Jian Jin, Bryan Roth and Stephen Frye, Publication date: 2011-07-01. 10. US 8071786 Indole compounds useful as serotonin selective agents. Howard P. Sard, Louis Shuster, Bryan Roth, Cynthia Morency, Govindaraj Kumaran, Liang Xu. Publication date: 2009-12-14 11. WO 2011097336 A2 HIGHLY SELECTIVE 5-HT(2C) RECEPTOR AGONISTS HAVING ANTAGONIST ACTIVITY AT THE 5-HT(2B) RECEPTOR, Alan Kozikowski, Bryan Roth, Andreas Svennebring,GangChen,CHO,Sung,Jin,Publicationdate:2011-02-0312. CA 2788416 A1 HIGHLY SELECTIVE 5-HT(2C) RECEPTOR AGONISTS HAVING ANTAGONIST ACTIVITY AT THE 5-HT(2B) RECEPTOR, Alan Kozikowski, Bryan Roth, Andreas Svennebring, Gang Chen, CHO, Sung, Jin, Publication date: 2011-02-03 13. EP 2254865 A1 INDOLE COMPOUNDS AND METHODS OF USE THEREOF, Howard P. Sard, Yiliang Zhang, Jie Li, Louis Shuster, Bryan Roth, Niels Jensen, Publication date: 2009-02-11. 14. WO 2010037050 A2 SYNTHESIS OF FUNCTIONALIZED OCTAHYDRO-ISOQUINOLIN-1-ONE-8-CARBOXAMIDES, OCTAHYDRO-ISOQUINOLIN-1-ONE-8-CARBOXYLIC ESTERS AND ANALOGS, AND THERAPEUTIC METHODS Jeffrey Aube, Bryan L. Roth, Partha Ghosh, Kevin J. Frankowski, Publication date: 2009-09-28 15. US 7687538 Agents with selective κ-opioid receptor affinity Jordan Zjawiony, Hesham Fahmy, David Jeremy Stewart, Bryan Roth Publication date: Publication date: 2005-07-29 16. US 7655691 Indole compounds useful as serotonin selective agents. Howard P. Sard, Louis Shuster, Bryan Roth, Cynthia Morency, Govindaraj Kumaran, Liang Xu, Publication date: 2005-09-27 17. CA 2353962 C SELECTIVE 5-HT6 RECEPTOR LIGANDS. Richard A. Glennon and Bryan L. Roth Publication date: 1999-12-10 18. CA 2715282 A1 INDOLE COMPOUNDS AND METHODS OF USE THEREOF, Howard P. Sard, Yiliang Zhang, Jie Li, Louis Shuster, Bryan Roth, Niels Jensen, Publication date: 2009-02-11 19. AU 2009214724 A1 INDOLE COMPOUNDS AND METHODS OF USE THEREOF, Howard P. Sard, Yiliang Zhang, Jie Li, Louis Shuster, Bryan Roth, Niels Jensen, Publication date: 2009-02-11

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20. WO 2009102805 A1 INDOLE COMPOUNDS AND METHODS OF USE THEREOF, Howard P. Sard, Yiliang Zhang, Jie Li, Louis Shuster, Bryan Roth, Niels Jensen, Publication date: 2009-02-11 21. US 20090203750 5-HT2C Receptor Agonists as Anorectic Agents Alan Kozikowski, Toru Kurome, Vincent Setola, Bryan Roth, Publication date: 2006-08-24 22. EP 1799640 A2 Indole compounds useful as serotonin selective agents. Howard P. Sard, Louis Shuster, Bryan Roth, Cynthia Morency, Govindaraj Kumaran, Liang Xu, Publication date: 2005-09-27 23. WO 2007025144 A1 5-HT2C Receptor Agonists as Anorectic Agents Alan Kozikowski, Toru Kurome, Vincent Setola, Bryan Roth, Publication date: 2006-08-24 24. ES 2260958 T3 LIGANDOS SELECTIVOS DEL RECEPTOR 5 - HT 6. Richard A. Glennon and Bryan L. Roth Publication date: 1999-12-10 25. EP 1693366 A1 SELECTIVE 5-HT6 RECEPTOR LIGANDS. Richard A. Glennon and Bryan L. Roth Publication date: 1999-12-10 26. PT 1149078 E LIGANDOS RECEPTORES DE 5-HT6 SELECTIVOS Richard A. Glennon and Bryan L. Roth Publication date: 1999-12-10 27. CA 2582079 A1 Indole compounds useful as serotonin selective agents. Howard P. Sard, Louis Shuster, Bryan Roth, Cynthia Morency, Govindaraj Kumaran, Liang Xu, Publication date: 2005-09-27 28. DK 1149078 T3 Selektive 5-HT6-receptorligander Richard A. Glennon and Bryan L. Roth Publication date: 1999-12-10 29. AU 2005300045 A1 A1 Indole compounds useful as serotonin selective agents. Howard P. Sard, Louis Shuster, Bryan Roth, Cynthia Morency, Govindaraj Kumaran, Liang Xu, Publication date: 2005-09-27 30. WO 2006047032 A2 A1 Indole compounds useful as serotonin selective agents. Howard P. Sard, Louis Shuster, Bryan Roth, Cynthia Morency, Govindaraj Kumaran, Liang Xu, Publication date: 2005-09-27 31. AT 319683 T SELEKTIVE 5-HT 6-REZEPTOR-LIGANDEN Richard A. Glennon and Bryan L. Roth Publication date: 1999-12-10 32. EP 1149078 B1 SELECTIVE 5-HT6 RECEPTOR LIGANDS. Richard A. Glennon and Bryan L. Roth Publication date: 1999-12-10 33. WO 2006012643 A2 Agents with selective κ-opioid receptor affinity Jordan Zjawiony, Hesham Fahmy, David Jeremy Stewart, Bryan Roth Publication date: Publication date: 2005-07-29

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34. AU 767009 B2 SELECTIVE 5-HT6 RECEPTOR LIGANDS. Richard A. Glennon and Bryan L. Roth Publication date: 1999-12-10 35. US 6518297 SELECTIVE 5-HT6 RECEPTOR LIGANDS. Richard A. Glennon and Bryan L. Roth Publication date: 2002-01-11 36. US 6489488 SELECTIVE 5-HT6 RECEPTOR LIGANDS. Richard A. Glennon and Bryan L. Roth Publication date: 2002-01-11 37. MX PA1005905 A SELECTIVE 5-HT6 Richard A. Glennon and Bryan L. Roth Publication date: 2001-06-11 38. US 6403808 SELECTIVE 5-HT6 RECEPTOR LIGANDS. Richard A. Glennon and Bryan L. Roth Publication date: 2001-08-20 39. WO 34242 A1 SELECTIVE 5-HT6 RECEPTOR LIGANDS. Richard A. Glennon and Bryan L. Roth Publication date: 1999-12-10 “5-HT6 selective antagonists” 40. WO2017007695A1 Mu opioid receptor modulators. Bryan L Roth, Daniela Gisela Dengler, Brian K Shoichet, Henry Lin, Peter Gmeiner, Aashish Manglik, Brian Kobilka. 2015-07-09 COMPANIES FOUNDED Founder and Chief Scientific Officer for Primax Biopharmaceuticals (formerly Primascreen, Inc) 2001-2003. Co-founder Epiodyne, Inc 2016-present AWARDS, HONORS, NAMED AND PLENARY LECTURES

Institute of Medicine/National Academy of Medicine of the National Academy of Sciences 2014-present Thompson Reuters Highly Cited Researcher: Pharmacology 2016, 2017 Thompson Reuters Highly Cited Researcher: Biology and Biochemistry 2015, 2017 Thompson Reuters ‘World’s Most Influential Scientific Minds’ 2015 Goodman and Gilman Award for Receptor Pharmacology—ASPET 2016 IUPHAR Analytcal Pharmacology Lecture (Announced 2018) Sigma-Aldrich Lecture ( St. Louis University and Sigma-Aldritch)--2017 Martin Rodbell Memorial Lecture (NIEHS/NIH)--2017 Pritchard Memorial Lecture, University of Maryland 2016 Keynote Lecture, CWRU Pharmacology Retreat 2016 Strongwater Endowed Lecture, Rutgers, 2016 Goodman Lecture, Portland, Oregon 2015

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Koppanyi Lecture, Georgetown University 2015 Philip S. Portoghese Lecture, Minneapolis 2015 Hyman Niznik Lecture, Quebec 2014 Swammerdam Lecture, Amsterdam 2014 Plenary Lecture EAPCCT, Brussels 2014 Keynote Lecture Fifth Annual Neurosciences Research Day University Hospitals of Cleveland (Case Western Reserve University) Cleveland, 2014 Special Lecture Society of Neurosciences “Chemical and Synthetic Neurobiology” 2013 Plenary Lecturer, International Society of Psychiatric Genetics, Hamburg Germany, 2012 Distinguished Lecturer, University of Toronto Neurosciences, Nov 2012 Keynote Lecturer International Narcotics Research Conference July 2012 PhRMA Foundation Excellence in Pharmacology Award, April 2011 Irving Page Lecture, Serotonin Club, July 2010 Lowenthal Lecture, MCV Neuroscience and School of Pharmacy; March 2010 Plenary Lecture, 10th Annual Frontiers in Neurosciences Retreat, Medical University of South Carolina, March 2009. NARSAD Distinguished Investigator Award, 2008 Plenary Lecture, Roche Pharmaceutical Global Medicinal Chemistry and

Safety, 2007 Prestige Lecturer, Universitie Montreal, 2007 Michael Hooker Chair of Protein Therapeutics and Translational Proteomics, UNC

Chapel Hill Medical School 2007- Steven G. Ferguson Memorial Lecture, Robarts Institute, Ontario Canada, 2006

Distinguished Lecture Series, Biomedical Sciences Training Program, Yale University Department of Psychiatry, April, 2005

Chauncy Leake Memorial Lecturer, Department of Pharmacology, University of Texas Medical Branch—Galveston, April, 2005.

Member of NARSAD Scientific Advisory Board (2004-) Heffter Research Institute Award for Outstanding Basic Science Research 1999

Career Development Award (KO2), National Institute of Mental Health 1996-2001 Career Development Award (KO2), National Institute of Mental Health 2001-2006 NARSAD Independent Investigator Award (1998-2000) Program Committee for Society of Neurosciences Annual Meeting 1995-1998 Sandoz Investigator (NARSAD), 1992-1994 NARSAD Young Investigator Award 1992-1994 American College of Neuropsychopharmacology Travel Awardee 1990 Dana Foundation Fellowship in Neuroscience (Stanford University) 1989-91 Naval Commendation Medal, 1989

Phi Beta Kappa, 1983 Delta Epsilon Sigma, 1977

March of Dimes Summer Research Fellowship, 1978 EDITORIAL BOARDS

Deputy Editor: Journal of Clinical Investigation (2014-2017) Associate Editor: Journal of Pharmacology and Experimental Therapeutics 2005- 2011 Associate Editor: Journal of Clinical Investigation (2012-2014)

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Handling Editor: Journal of Neurochemistry 2000-2008 Associate Editor: Pharmacology and Therapeutics 2000-2006 Journal of Pharmacology and Experimental Therapeutics 1998-present Medicinal Chemistry Research 1996-present Journal of Biological Chemistry 2001-2006 Psychopharmacology 1998-present Neuropsychopharmacology 1999-2002 Journal of Receptors and Signal Transduction 2002-present Molecular Pharmacology 2006- ACS Medicinal Chemistry Letters 2010- Faculty of 1000 (2010-)

Biochemistry (2017-) Guest Editor PNAS 2009; 2015

EDITORIAL REFEREE

Science Science Signaling Science Translational Medicine Science Advances Nature Nature Biotechnology Nature Neurosciences Nature Chemical Biology Nature Structural and Molecular Biology Nature Cell Biology Nature Reviews Neurosciences Nature Reviews Drug Discovery Nature Nanotechnology Nature Chemistry Nature Methods Cell Neuron Cell Reports Proceedings of the National Academy of Sciences, USA PLOS Biology Trends in Pharmacological Sciences Trends in Neurosciences The Journal of Biological Chemistry Biochemistry The Journal of Neurosciences Molecular Pharmacology The Journal of Pharmacology and Experimental Therapeutics The Journal of Neurochemistry Biochemical Pharmacology American Journal of Psychiatry Brain Research Developmental Brain Research Peptides

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Brain Research Bulletin Pharmacology, Biochemistry and Behavior Experimental Neurology The Journal of Clinical Investigation The European Journal of Pharmacology The European Journal of Pharmacology: Molecular Pharmacology Section Neuropsychopharmacology Synapse Molecular Endocrinology The Journal of Cardiovascular Pharmacology The Journal of Molecular and Cellular Cardiology Circulatory Shock Neuropharmacology Neurology Biological Psychiatry Drugs Medicinal Chemistry Research Psychopharmacology Life Sciences Neuropsychiatric Genetics Molecular Psychiatry Pharmacology and Therapeutics Journal of Neuroimmunology

STUDY SECTIONS AND NIH ADVISORY PANELS (Incomplete list)

Regular Member, Neurochemistry-Neuropharmacology Study Section, NIMH 1996-1998

Regular Member, Molecular, Cellular and Developmental Neurobiology #5, DRG/NIH; 1998-2000 Regular Member, Molecular, Cellular and Developmental Neurobiology #5, DRG/NIH 2001-2003. Regular Member, Molecular Neurochemistry and Pharmacology Study Section, DRG/NIH, 2003-2004. Regular Member, Molecular Neuropharmacology and Signaling Study Section, DRG/NIH 2006-2009. Reviewer Ad Hoc Pharmacogenomics Study Section, 2001. Chair Molecular Libraries Screening Centers Special Review Group, 2004 Chair Molecular Libraries HTS Assay Development Special Review Group, July 2005 Chair Molecular Libraries HTS Assay Development Special Review Group, March 2006-2007 Scientific Advisor: Molecular Libriaries Initiative (2006-2011); MLI Mid-Course Review Committee (2006); Molecular Libraries Probe Center Network 2008-2011. Scientific Advisor: NIH Neurotherapeutics Initiative (2011-2014) Ad hoc reviewer and others (partial list; typically I participate in at least 3 NIH review

groups/year) NIMH Board of Scientific Counsellors, Nov., 1997 ad hoc NIMH Board of Scientific Counsellors, Nov., 2003 ad hoc NIMH Board of scientific Counsellors, Sept 2008 ad hoc NINDS Board of Scientific Counsellors, 2010, 2015, ad hoc

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Member Scientific Organizing Committee for the NIH Roadmap Workshop on Predictive Toxicology and ADME; 2004 Ad Hoc Reviewer, VA Merit Review Board for Basic Sciences, 1992 Ad Hoc Reviewer, VA Merit Review Board for Neurosciences, 1994 External Reviewer, VA Career Development Board, 1995 Member, VA Grant Review Board, Cleveland VAMC, Cleveland, OH 1993- 1995 Ad Hoc Reviewer, Frontiers International Visiting Scientists Program, 1995 Special Reviewer, MCDN Study Section, Special Emphasis Panel,NIMH,1995 Special Reviewer, Neurochemistry-Neuropharmacology Study Section, NIMH,

--October 13-14, 1995--March 21-22, 1996 Member, Special Emphasis Panel, NHLBI, April 23-24, 1996 Special Emphasis Panel, NIMH, October 22, 1996 Outside Reviewer-Biochemistry Study Section, DRG, Oct. 1996. Special Emphasis Panel, NIMH, March 24, 1997 Outside Reviewer-Molecular, Cellular and Developmental Biology Study Section -NIMH, Feb 24, 1997 Reverse Site Visit, NIA, April, 1997 Special Emphasis Panel, NINDS, June 19-20, 1997 Special Emphasis Panel, NIMH, July 15, 1997 Special Emphasis Panel, NIMH, August 8, 1997. Ad Hoc Reviewer, NIMH Board of Scientific Counselors Meeting, Oct. 1997. Ad Hoc Reviewer, NSF Ad Hoc Reviewer, NIMH, October 1998. External Advisor: NIH Molecular Imaging Roadmap - Imaging Database implementation group; 2004-2008

SCIENTIFIC SOCIETIES

Society for the Neurosciences, 1985-2007; 2015-present Serotonin Club, 1986-present American Society of Pharmacology and Experimental Therapeutics 2000-2013; 2015- present American Society for Biochemistry and Molecular Biology 2001-2008 American College of Neuropsychopharmacology (2005-2013)

MEDICAL LICENSE

Licensed in the State of California, 1988-1992 (G065075) DEA License (BR2093451) Diplomate of the National Board of Medical Examiners (247821) Licensed in the State of Ohio, 1991-2007 (61679)

MEDICAL EXPERIENCE

1989-1991 Santa Clara Valley Medical Center, Emergency Psychiatric Services, San Jose, CA: Extra help psychiatrist, 40-64 hours/month.

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1991-present Ward Attending, Schizophrenia Research Ward, Hanna Pavilion 3, University Hospitals of Cleveland, Case Western Reserve University School of Medicine.

1993-1994 Ward Chief, Schizophrenia Research Ward, Hanna Pavilion 3, University Hospitals of Cleveland, Case Western Reserve University School of Medicine.

1994-2001 Ward Attending, HP-4, University Hospitals of Cleveland, Case Western

Reserve University School of Medicine. CONFERENCES CHAIRED OR ORGANIZED 1987-1988 Chairman and organizer: "Molecular and Cellular Mechanisms of Septic Shock" (Held in Bethesda, MD March 31-April 1, 1988) 1989 Co-Chairman: "Serotonin Receptors: molecular neurobiology and physiology" American College of Neuropsychopharmacology Annual Meeting (Maui, Hawaii, December, 1989) 1990 Session Chairman: "Molecular Neurobiology of 5HT Receptors", Society of Neurosciences Annual Meeting. 1991 Session Chairman: "5HT Receptors", Society of Neurosciences Annual Meeting. 1992 Organizer: Special Interest Dinner for Psychopharmacology, Society of Neurosciences Annual Meeting. 1992 Session Chairman: "Neuropharmacology of Serotonin", Society of Neurosciences Annual Meeting. 1995-1998 Member Program Committee, Society of Neurosciences Annual Meeting 1996 Co-Chair, “New Insights into Receptor Regulation” American College of Neuropsychopharmacology Annual Meeting, December 1996. 1997 Session Chairman: “Psychopharmacology: General”, Society of Neurosciences Annual Meeting. 1998 Organizer: IUPHAR Satellite Symposium on ”Novel mechanisms of serotonin receptor

signal transduction”, Rotterdam, July, 1998. 1999 Session Chairman: “Neurochemical Imaging” International Congress on Schizophrenia Research, Santa Fe, NM. April, 1999. June 2000—session co-chair Pharmacological Approaches to Functional Mouse Genomics; NIMH/NIDA Panel on Functional Mouse Genomics, Virginia. October 2001; 2002: Program Committee Great Lakes GPCR Meeting November 2001: Session Chair: ‘Serotonin and purinergic receptors’ Society for Neurosciences Annual Meeting, Nov, 2001.

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April 2003: Organizer of Symposium on 5-HT2-family receptors for FASEB/ASPET meeting, San Diego, CA. 2004: Member Scientific Organizing Committee for the NIH Roadmap Workshop on Predictive Toxicology and ADME 2004: Co-Chair on novel mechanisms for drug discovery. ACNP Annual Meeting, Puerto Rico, Dec. 2004. 2005: Organizer of Symposium on Molecular Libraries for CNS Drug Discovery for ASPET/FASEB meeting. 2005: Organizer of Panel on Lipid Rafts at ACNP Annual Meeting, Hawaii. 2005: Co-Chair of Symposium on Lipid Rafts and Caveolin, Society for Neurosciences Annual Meeting. 2006: Co-Chair of Symposium on Allosterism and GPCR signaling; FASEB Meeting, ASPET 2006. 2006: Chair of CINP Symposium on Atypical antipsychotic drugs: what confers atypicality? 2006: Chair of 5-HT receptor symposium, International Serotonin Club Meeting (Japan, June 2006): 5-HT receptor interacting proteins. 2006: Chair of ACNP Symposium on k-opioid receptors and mood disorders therapeutics. 2006 ACNP Annual Meeting. 2007: Co-Chair ACNP Symposium on Neuroengineering. 2007 ACNP Annual Meeting. 2008: Emerging Themes in GPCR Signaling. Madison Wisconsin, Sept 9-10. 2011: NYAS Advancing Drug Discovery in Schizophrenia, March 9-11 2014: NYAS GPCR Functional Selectivity, September 30, 2014 PUBLICATIONS (BOOKS)

1 BL Roth, T Nielsen, and AE McKee (Eds): Molecular and cellular mechanisms of septic shock. (New York: Alan R. Liss), 1989.

2 BL Roth (Editor): The 5-HT receptors (Human Press), April 2006. PUBLICATIONS (MANUSCRIPTS) 1 CJ Coscia, WJ Burke, MP Galloway, AH Kosloff, J McFarlane, JS Mitchell and BL Roth:

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Effects of norlaudanosoline carboxylic acids on enzymes of catecholamine metabolism. J Pharm Exp Ther 212:91-96, 1980. 2 BL Roth, MP Galloway and CJ Coscia: The effects of morphine on catecholamine metabolism during postnatal development. Brain Res 197:561-564, 1980. 3 MP Galloway, BL Roth and CJ Coscia: The effects of tetrahydroisoquinolinecarboxylic acids on tyrosine-3-monooxygenase. Arch Biochem Biophys 209: 620-627, 1981. 4 BL Roth, MB Laskowski and CJ Coscia: Evidence for distinct subcellular sites of opiate receptors. J Biol Chem 256:10117-10123, 1981. 5 BL Roth, MB Laskowski and CJ Coscia: Microsomal opiate receptors differ from synaptic membrane receptors in proteolytic sensitivity. Brain Res 250: 101-109, 1982. 6 MW Wohltmann, BL Roth, and CJ Coscia: Differential postnatal development of mu and delta opiate receptors. Devel Brain Res 3:679-684, 1982. 7 KG Pryhuber, BL Roth and CJ Coscia: Demonstration of a slowly dissociating form of bovine hippocampal synaptic membrane opiate receptor. Eur J Pharm 83:47-53, 1982. 8 BL Roth: Microsomal and synaptic membrane opiate receptors. PhD Thesis, St. Louis University School of Medicine, Department of Biochemistry, 1983. 9 JW Spain, DB Bennett, BL Roth and CJ Coscia: Ontogeny of benzomorphan-selective sites (k): a computerized analysis. Life Sci (Suppl I) 33:235-239, 1983. 10 BL Roth, DB Bennett, K Pryhuber, S Scheibe and CJ Coscia: A slowly dissociating form of bovine hippocampus opiate receptor. In: Membrane Located Receptors for Drugs and Endogenous Agents, Methodological Surveys in Biochemistry and Analysis, Vol 13 (E Reed, GMW Cook and DJ Morre, Eds) (New York: Plenum Press), 1984. 11 BL Roth, MC Beinfeld and AC Howlett: Secretin receptors on neuroblastoma cell membranes: characterization of 125I-labeled secretin binding and association with adenylate cyclase. J Neurochem 42:1145- 1152, 1984. 12 BL Roth and CJ Coscia: Microsomal opiate receptors:characterization of smooth microsomal and synaptic membrane opiate receptors. J Neurochem 42: 1677-1684, 1984. 13 MC Beinfeld, DM Korchak, BL Roth and T O'Donohue: The distribution and chromatographic characterization of PHI (Peptide Histidine Isoleucine Amide) -27-like peptides in rat and porcine brain. J Neurosci 4:2681-2688, 1984. 14 SD Scheibe, DB Bennett, JW Spain, BL Roth and CJ Coscia: Kinetic evidence for differential agonist and antagonist binding to bovine hippocampal synaptic membrane opiate receptors. J Biol Chem 259:3298-3303, 1984. 15 BL Roth, T Nakaki, D-M Chuang and E Costa: Aortic recognition sites for serotonin (5HT) are coupled to phospholipase C and modulate phosphatidylinositol turnover.

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Neuropharm 23:1223-1226, 1984. 16 JW Spain, BL Roth and CJ Coscia: Differential ontogeny of multiple opioid receptors ( µ, d, k) J Neurosci 5:584-588, 1985. 17 DB Bennett, JW Spain, MB Laskowski, BL Roth and CJ Coscia: Stereospecific opiate binding sites occur in coated vesicles. J Neurosci 5: 3010-3015, 1985. 18 BL Roth, T Nakaki, D-M Chuang and E Costa: Evidence for an endacoid for the 5HT2 recognition site. In: Proceedings of the First International Symposium on Endacoids, Progress in Clinical and Biological Research H. Lal, Ed. (New York: Alan R. Liss), 1985. 19 T.Nakaki, BL Roth, D-M Chuang and E Costa: 5-hydroxytryptamine uptake and imipramine binding sites in neurotumor NCB-20 cells. J Neurochem 45:920-925, 1985. 20 BL Roth and MC Beinfeld: Postnatal development of VIP binding sites in rat forebrain and hindbrain. Peptides 6:27-30, 1985. 21 T Nakaki, BL Roth, D-M Chuang and E Costa: Phasic and tonic components in 5HT2 receptor mediated rat aorta contraction: participation of Ca++ channels and phospholipase C. J Pharm Exp Ther 234:442-446, 1985. 22 E Legan, J Parillo, B Chernow and BL Roth: Activation of phosphatidylinositol turnover in rat aorta by alpha1-adrenergic receptor stimulation. Eur J Pharm 110:389- 390, 1985. 23 F Nicoletti, J Meek, MJ Iadarola, D-M Chuang, BL Roth and E Costa: Coupling of inositol phospholipid metabolism with excitatory amino acid recognition sites in rat hippocampus. J Neurochem 46:40-46,1986. 24 B Chernow and BL Roth: Pharmacologic support of the cardiovasculature in septic shock. In: Proceedings of the New Horizon's Focus Group on Septic Shock. (Sibbald and Schumer, Eds) (Fullerton CA: Critical Care Medicine), Chapter 11, 1986. 25 B Chernow and BL Roth: Pharmacologic manipulation of the peripheral vasculature in shock: clinical and experimental approaches Circ Shock 18:141-155, 1986. 26 M McMillan, B Chernow and BL Roth: Hepatic alpha1-adrenergic receptor alteration in a rat model of chronic sepsis. Circ Shock 19:185-194,1986. 27 M McMillan, B Chernow and BL Roth: Phorbol esters inhibit alpha1-adrenergic receptor-stimulated phosphoinositide hydrolysis and contraction in rat aorta: evidence for a link between vascular contraction and phosphoinositide metabolism. Biochem Biophys Res Comm 134:970-974, 1986. 28 N Ives, JW King, B Chernow and BL Roth: BAY k 8644, a calcium channel agonist, reverses hypotension in endotoxin shocked rats. Eur J Pharm 130:169-175, 1986. 29 BL Roth, T Nakaki, D-M Chuang and E Costa: Characterization of 5HT2 receptors linked to phospholipase C in rat aorta: modulation of phosphoinositide hydrolysis by phorbol

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ester. J Pharm Exp Ther 238:480-485, 1986. 30 D-M Chuang, O Carter, JW Spain, MB Laskowski, BL Roth, and CJ Coscia: Detection and characterization of b-adrenergic receptors and adenylate cyclase in coated vesicles isolated from bovine brain. J Neurosci 6:2578 -2584, 1986. 31 JA Spitzer, E Turco, I Deaucic and BL Roth: Perturbations of transmembrane signaling mechanisms in acute and chronic endotoxemia. In: 1st Vienna Shock Society Proceedings (New York: Alan R. Liss), 401-418, 1987. 32 EA Suba and BL Roth: Prostaglandins activate phosphoinositide metabolism in rat aorta. Eur J Pharm 136: 325- 332, 1987. 33 BL Roth and JA Spitzer: Altered hepatic vasopressin and alpha1-adrenergic receptors after chronic endotoxin infusion. Am J Physiol 252:E699-E702, 1987. 34 BL Roth, J Disimone, EA Majane and H-Y T Yang: Elevation of arterial pressure in rats by two new vertebrate peptides FLFQPQRF-NH2 and AGEGLSSPFWSLAAPQRRF-NH2 which are immunoreactive to FMRF-NH2 antiserum. Neuropeptides 10:37-42, 1987. 35 BL Roth: Modulation of phosphatidylinositol-4,5-bis-phosphate hydrolysis in rat aorta by guanine nucleotides, calcium and magnesium in rat aorta. Life Sci 41:629-634, 1987. 36 BL Roth and D-M Chuang: Minireview: multiple mechanisms of serotonergic signal transduction. Life Sci 41:1051-1064, 1987. 37 BL Roth, S McLean, X-Z Zhu and D-M Chuang: Characterization of two [3H]-ketanserin recognition sites in rat striatum. J Neurochem 49:1833-1838, 1987. 38 RZ Litten, EA Suba and BL Roth: Effects of a phorbol ester on rat aorta contraction and calcium influx in the presence and absence of BAY k 8644. Eur J Pharm 144:185-191, 1987. 39 RZ Litten, JC Carcillo and BL Roth: Alterations in bidirectional transmembrane calcium flux occur without changes in protein kinase C levels in rat aorta during intraperitoneal sepsis. Circ Shock, 25:123-130, 1988. 40 JC Carcillo, RZ Litten, EA Suba and BL Roth: Alterations in rat aortic alpha1-adrenoceptors and alpha1-adrenergic stimulated phosphoinositide hydrolysis in intraperitoneal sepsis, Circ Shock, 26:331-339, 1988. 41 BL Roth, EA Suba, JA Carcillo and RZ Litten: Alterations in hepatic and aortic phospholipase C-coupled receptors and signal transduction in rat intraperitoneal sepsis, Prog Clin Biol Res, 286: 41-59, 1989. 42 JA Carcillo, RZ Litten and BL Roth: Norepinephrine-induced phosphorylation of a 25-Kda protein in rat aorta during intraperitoneal sepsis. Circ Shock, 28: 257-265, 1989. 43 JB Hermiller, I Deuciuc, JA Spitzer and BL Roth: Alteration of hepatic and splenic protein kinase C in sepsis and chronic endotoxemia. IN: Molecular and Cellular Mechanisms of

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Septic Shock (BL Roth, T Nielssen and AE McKee, eds) (New York: Alan R Liss), 61-70, 1989. 44 BL Roth, J Mehegan , D Jacabowitz, F Robey and MJ Iadarola: Rat Brain Protein Kinase C: purification, antibody production and quantification in discrete regions of hippocampus, J. Neurochem, 52:215-221, 1989. 45 S McLean, RB Rothman, D-M Chuang , K Rice, JW Spain, CJ Coscia and BL Roth: Cross-linking of [125I]b-endorphin to µ-opioid receptors during development. Devel Brain Res, 45:283-289, 1989. 46 JA Spitzer, IV Deaciuc, EB Rodriguez de Turco, BL Roth, JB Hermiller and JP Mehegan: Modification of protein kinase C(PKC) activity and diacylglycerol (DAG) accumulation in hepatocytes in continuous endotoxemia. Second Vienna Shock Forum Proceedings (New York: Alan R Liss), 575-588, 1989. 47 JA Spitzer, EB Rodriguez de Turco, IV Deaciuc, BL Roth, JB Hermiller and JP Mehegan: Receptor changes in endotoxemia. Perspectives in Shock Research, (New York: Alan R. Liss), 95-106, 1989. 48 BL Roth, MJ Iadarola , J Mehegan and DA Jacobowitz: Immunohistochemical distribution of B-protein kinase C in rat hippocampus determined with an antibody against a synthetic peptide sequence. Brain Res Bull, 22: 893-897, 1989. 49 BL Roth: Role of phosphoinositide hydrolysis and protein kinase C activation in smooth muscle function. IN: SEROTONIN: from cell biology to pharmacology and therapeutics (Kluwer Academic Press), 33-37, 1990. 50 MR Seggal, MY Youssif, RA Lyons, M Titler, BL Roth, EA Suba and RA Glennon: A structure--affinity study of the binding of 4-substituted analogues of 1-(2,5-dimethoxyphenyl)-2-aminopropane at the 5HT2 serotonin receptors, J Med Chem, 33: 1032-1036, 1990. 51. BL Roth, Review of "Clinical pharmacology in psychiatry: from molecular studies to clinical reality", Neuropsychopharm, 4: 283-284, 1991. 52 BL Roth, MW Hamblin, R Desai and RD Ciaranello: Developmental and synaptic regulation of 5HT2 and 5HT1c serotonin receptors, In: Serotonin: molecular biology, receptors and functional effects (Fozard and Saxena, Eds) 31-42, 1991. 53 BL Roth, MD Hamblin and RD Ciaranello: Regulation of 5HT2 and 5HT1c receptor levels: methodology and mechanisms, Neuropsychopharmacology, 3:427-433,1990. 54 BL Roth, M Hamblin and RD Ciaranello: Developmental regulation of 5HT1c and 5HT2 mRNA and receptor levels, Devel Brain Res, 58: 51-58,1991. 55 BL Roth and RD Ciaranello: Molecular biology of the brain, 10th Annual APA Yearbook, Tasman and Goldfinger (Eds), 404-422, 1991. 56 BL Roth and RD Ciaranello: Chronic mianserin treatment decreases 5-HT2 receptor binding without altering 5-HT2 receptor mRNA levels. Eur J Pharm, (Mol Pharm Section),

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207:169-172, 1991. 57 S Garlow, D Morilak, R Dean, BL Roth and RD Ciaranello: Production and characterization of a 5-HT2 receptor antibody. Brain Res, 615: 113-120,1993. 58 BL Roth, RD Ciaranello and HY Meltzer: Binding of typical and atypical antipsychotic agents to transiently expressed 5HT1c receptors. J Pharm Exp Ther, 260: 1361-1366, 1992. 59 MS. Choudhary, S. Craigo and BL Roth: Identification of receptor domains which modify ligand binding to 5-hydroxytryptamine2 and 5-hydroxytryptamine1c serotonin receptors. Mol Pharm, 42:627-633,1992. 60 BL Roth: Multiple serotonin receptors: clinical and experimental aspects, Annals of Clin Psych, 6:67-78,1994. 61 BL Roth, S Craigo and S Choudhary: Chimeric receptor proteins as tools for medicinal chemists. Medicinal Chemistry Research, 2:229-241, 1992 (Invited Review). 62 MS. Choudhary, S. Craigo and BL Roth: A single point mutation (Phe340->Leu340) of a conserved phenylalanine abolishes 4-[125I]-iodo-(2,5-dimethoxy)phenylisopropylamine and [3H]-mesulergine but not [3H]-ketanserin binding to 5-hydroxytryptamine2 receptors. Mol Pharmacol, 43: 755-761, 1993. 63 RD Ciaranello, J Ami, R Dean, R Desai, S Garlow, MR Heller, D Morilak and BL Roth. Psychopharmacol Ser (LF Gram, LP Balant, HY Meltzer and SG Dahl, Eds) (Berlin: Springer-Verlag),10: 26-37, 1993. 64 BL Roth and HY Meltzer: The role of serotonin in schizophrenia. In: Psychopharmacology, The 4th Generation of Progress (Eds. F Bloom and DJ Kupfer), 1215-1227, 1995. 65 MS Choudhary, AZ Uluer, N Sachs, RA Glennon, RB Westkaemper and BL Roth: Differential ergoline and ergopeptine binding to 5-hydroxytryptamine2A receptors: ergolines require an aromatic residue at position 340 for high affinity binding. Mol Pharmacol., 47: 450-457, 1995. 66 B L. Roth, S C. Craigo, M. S Choudhary, A. Uluer, F J. Monsma, Jr, Y. Shen, H Y. Meltzer, and D R. Sibley: Binding of typical and atypical antipsychotic agetns to 5-hydroxytryptamine (5-HT6) and 5-hydroxytryptamine7 (5-HT7) receptors. J Pharmacol Exp Ther. 268: 1403-1410,1994. 67 BL Roth, S Choudhary and S Craigo: Mutagenesis of 5-HT2 serotonin receptors: what does an analysis of many mutant receptors tell us? Med Chem Res, 3:297-305, 1994. 68 S Fatemi, HY Meltzer and BL Roth: Atypical antipsychotic drugs: clinical and experimental aspects. Chapter 4 in: "Antipsychotics", Handbook of Experimental Pharmacology, v. 120, pp. 77-116, editor, J.G. Csernansky, Berlin ; New York : Springer, 1996. 69 JF Nash, BL Roth, JD Brodkin, DE Nichols, GA Gudelsky: Effect of the R(-) and S(+)

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isomers of MDA and MDMA on phosphatidylinositol turnover in cultured cells expressing 5-HT2A or 5-HT2C receptors. Neurosci Lett,177: 111-115, 1994. 70 DE Nichols, S Frescas, D Marona-Lewicka, X Huang, BL Roth, GA Gudelsky and JF Nash: 1-(2,5-Dimethoxy-4-trifluoromethylphenyl)-2-aminopropane: a potent serotonin 5-HT2A/2C agonist. J Med Chem, 37: 4346-4351, 1994. 71 BL Roth, E Pekka-Palvimaki, S Berry, N Khan, N Sachs, A Uluer and MS Choudhary: 5-Hydroxytryptamine2A (5-HT2A) receptor desensitization can occur without downregulation. J Pharm Exp Thera, 275: 1638-1646, 1995. 72 R Kohen, MA Metcalf, N Khan, T Druck, K Huebner, JE Lachowicz, DR Sibley, BL Roth and MW Hamblin: Cloning, characterization and chromosomal localization of a human 5-HT6 serotonin receptor. J Neurochem, 66:47-56, 1996. 73 BL Roth, S Tandra, LH Burgess, DR Sibley and HY Meltzer: D4 dopamine receptor affinity does not distinguish between typical and atypical antipsychotic drugs. Psychopharmacol, 120: 365-368, 1995. 74 BL Roth, Serotonin as a neuromodulator. Chapter in: Clinical Psychopharmacology, (J Barchas, Ed), submitted. 75. E-P Palvimaki, BL Roth, H Majasuo, A Laakso, M Kuoppamaki, E Syvlahti and J Hietala: Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2C receptor, Psychopharmacol, 126: 234-240, 1996. 76. SA Berry, M Shah, N Khan and BL Roth: Rapid agonist induced internalization of 5-Hyroxytryptamine2A (5-HT2A) receptors occurs via endosomes in vitro. Mol Pharmacol,50: 306-313, 1996. 77. BL Roth, M Shoham, MS Choudhary and N Khan: Identification of highly conserved aromatic residues essential for agonist binding and second messenger production at 5-HT2A receptors. Mol Pharmacol, 52: 259-266, 1997. 78. BL Roth, MS Choudhary, N Khan, and AZ Uluer: High affinity agonist binding is not sufficient for agonist efficacy at 5-HT2A receptors:evidence in favor of a modified ternary complex model. J Pharm Exp Thera, 280: 576-583, 1997. 79. BL Roth and DR Sibley: COMMENTARY ON: Atypical neuroleptics have low affinity for dopamine D2 receptor or are selective for D4 by Seeman et al. Neuropsychopharmacol. 16: 114-115, 1997. 80. DA Willins, AY Deutsch and BL Roth: 5-HT2A receptors are expressed on pyramidal cells and interneurons in rat cortex. Synapse, 27:79-82, 1997. 81. BL Roth and EA Hyde: Pharmacology of 5-HT2 receptors, In: Serotonergic neruons and 5-HT receptors in the CNS (HG Baumgarten and M Gothert, Eds), 367-390, 1997. 82. RL Findling, BL Roth and SC Schulz: Risperidone: broadening clinical indications, In:

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The Art of Rational Risperidone Therapy (FJ Ayd, Ed), 21-44, 1997. 83. BL Roth, HY Meltzer and N Khan: Binding of typical and atypical antipsychotic drugs to multiple neurotransmitter receptors. In: Advances in Pharmacology (Vol. 42), D Goldstein, G Eisenhofer and R McCarthy eds. Academic Press, 482-485, 1998. 84. RB Westkaemper, RA Glennon, EA Hyde, MS Choudhary, N Khan, EI Gelber and BL Roth: Engineering in a region of bulk tolerance into the 5-HT2A receptor. Eur J Med Chem, 34: 441-447, 1999. 85. BL Roth, DA Willins, KR Kristiansen and W Kroeze: 5-HT2-family receptors (5-HT2A, 5-HT2B, 5-HT2C): where structure meets function. Pharmacology and Therapeutics, 79: 231-257, 1998. 86. WK Kroeze and BL Roth: Molecular biology of serotonin receptors: therapeutic implications for the interface of mood and psychosis. Biol Psych 44: 1128-1142, 1998. 87. DL Willins, L Alsayegh, SA Berry, J Backstrom, E Sanders-Bush, L Friedman, N Khan, and B L Roth: Clozapine and other 5-hydroxytryptamine2A receptor antagonists alter the subcellular distribution of 5-hydroxytryptamine-2A receptors in vitro and in vivo. Neurosci 91: 599-606, 1999. 88. DL Willins, L Alsayegh, SA Berry, J Backstrom, E Sanders-Bush, L Friedman, N Khan and BL Roth: Serotonergic antagonist effects on trafficking of serotonin 5-HT2A receptors in vitro and in vivo. Proceedings of the Conference on the Molecular Biology of Serotonin Receptors, New York Academy of Sciences, 861: 121-127, 1998. 89. BL Roth, DL Willins and WK Kroeze: G-protein coupled receptor (GPCR) trafficking in the central nervous system: relevance for drugs of abuse. Drug and Alcohol Abuse Res, 51:73-85, 1998. 90. BL Roth, SA Berry, DL Willins, K Kristiansen and WK Kroeze: Serotonin 5-HT2A receptors: molecular biology and mechanisms of regulation. Crit Rev Neurobiol 12: 319-338, 1998. 91. EI Gelber, WK Kroeze, DL Willins, J Gray, CA Sinar, E Hyde, V Gurevich, J Benovic and BL Roth: Structure and function of the third intracellular loop of the 5-HT2A receptor: the third intracellular loop is a-helical and binds purified arrestins. J Neurochem, 72: 2206-2214, 1999. 92. G Rajkowska, JJ Miguel-Hidalgo, J Wei, G Dilley, SD Pittman, HY Meltzer, JC Overholser, BL Roth and CA Stockmeier: Morphometric evidence for neuronal and glial prefrontal cell pathology in major depression. Biol Psych.45: 1085-1099, 1999. 93. P.-Z. Tan*, R. M. Baldwin, C. H. Van Dyck, M. -Al-Tikriti, B.L. Roth, N. Khan,D. S. Charney, and R. B. Innis: Characterization of radioactive metabolites of 5-HT2A receptor PET ligand [18F]Altanserin in human and rodent. Nucl. Med. Biol 26: 601-608, 1998. 94. Christina Egan, Ellinor Grinde, Ann DuPre, Bryan L. Roth, Michael Hake, Milt Teitler*,

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and Katharine Herrick-Davis. Agonist High and Low Affinity State Ratios Predict Drug Intrinsic Activity and a Revised Ternary Complex Mechanism at Serotonin 5-HT2A and 5-HT2C, Synapse,35: 144-150, 2000. 95. Richard B. Westkaemper, Scott P Runyon, Mikhail L. Bondarev, Jason E. Savage, Bryan L. Roth and Richard A. Glennon. 9-(Aminomethyl)-9,10-dihydroanthracene (AMDA) is a novel and unlikely 5-HT2A receptor antagonist. Eur J Pharmacol, 380: 125-127, 1999. 97. BL Roth, PF Buckley and SC Schulz: Molecular biology and antipsychotic medications, In: APA Annual Reviews of Psychiatry (CA Tamminga, Ed), 1999. 98. BL Roth: What’s all the RAVE about receptor internalization? Neuron, 23: 629-631, 1999. 99. RA Glennon, M Bondarev and BL Roth: 5HT6 serotonin receptor binding of indolealkylamines: a preliminary structure-affinity investigation. Med Chem Res 9: 108-117, 1999. 100. BL Roth, DL Willlins, K Kristiansen and WK Kroeze: Activation is hallucinogenic and antagonism is therapeutic: role of 5-HT2A receptors in atypical antipsychotic drug actions. The Neuroscientist 5: 254-262, 1999. 101. RA Glennon, M Lee, JB Rangisetty, M Dukat, BL Roth, J Savage, A McBride, L Rauser, S Hufasein, DKH Lee: 2-Substituted tryptamines: agents with selectivity for 5-HT6 serotonin receptors. J Med Chem. 43: 1011-1018. 2000. 102. K Kristiansen, WK Kroeze, DL Willins, EI Gelber, JE Savage, RA Glennon and BL Roth: A highly conserved aspartic acid (Asp-155) anchors the terminal amine moiety of tryptamines and is involved in membrane targeting of the 5-HT2A serotonin receptor but does not participate in activation via a ‘Salt-Bridge Disruption’ mechanism. J Pharm Exp Thera 293: 735-746, 2000. 103. BL Roth, WK Kroeze, S Platel and E Lopez: The Multiplicity of Serotonin Receptors: Uselessly diverse molecules or an embarrassment of riches? The Neuroscientist, 6: 252-262, 2000. 104. RB Rothman, MH Baumann, JE Savage, L Rauser, A McBride, S Hufisein and BL Roth: Evidence for Possible Involvement of 5-HT2B Receptors in the Cardiac Valvulopathy Associated with Fenfluramine and Other Serotonergic Medications, Circulation. 2000 Dec 5;102(23):2836-41. 105. DA Shapiro, K Kristiansen, WK Kroeze and BL Roth: Differential modes of agonist binding to 5-HT2A receptors revealed by mutations of transmembrane domain V. Mol Pharmacol. 2000 Nov;58(5):877-86. 106. A Bhatnagar, DL Willins, JA Gray, JL Benovic and BL Roth: The dynamin-dependent, arrestin-independent internalization of 5-HT2A serotonin receptors reveals differential sorting of arrestins and 5-HT2A receptors during endocytosis. J Biol Chem. (2000 epub Nov 7).276: 8269-8277, 2001.

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107. JE Piletz, TR Ivanov, JD Sharp, P Ernsberger, C-H Chang, RT Pckard, G Gold, B Roth, H Zhu, JC Jones, J Baldwin and DJ Reis: Imidazoline receptor antisera-selected (IRAS) cDNA: cloning and characterization. DNA and Cell Biol, 19: 319-329, 2000. 108. L Qiao, R Etcheberrigaray, AP Kozikowski, J Savage and BL Roth: A novel PKC activator enhances sAPP secretion in PC-12 cells. In press. 109. BL Roth: Neuronal Signal Transduction Pathways: Wasteland or the Promised Land? Science (STKE: http://www.stke.org/cgi/content/full/ OC_sigtrans;2000/45/pe1, 2000). 110. Tsai Y, Dukat M, Slassi A, MacLean N, Demchyshyn L, Savage JE, Roth BL, Hufesein S, Lee M, Glennon RA.N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonistst. Bioorg Med Chem Lett. 10(20):2295-9, 2000. 111. SP Runyon, JE Savage, M Taroua, BL Roth, RA Glennon and RB Westkaemper: Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene. Bioorg Med Chem Lett, 11:655-658, 2001. 112. RB Westkaemper, SP. Runyon, JE Savage, BL Roth, RA Glennon: Exploring the Relationship Between Binding Modes of 9-(Aminomethyl)-9,10-dihydroanthracene and Cyproheptadine Analogs at the 5-HT2A Serotonin Receptor, Bioorg Med Chem Lett, 11:563-566, 2001. 113. L Qiao, L-Y Zhao, S Rong, X-W Wu, S Wang, J Tan, RI Glazer, JE Savage, BL Roth, J Flippen-Anderson, and AP Kozikowski: Rational Design, Synthesis and Biological Evaluation of Rigid Pyrrolidone Analogs as Prostate Cancer Inhibitors, Bioorg Med Chem Lett, 11:955-959, 2001. 114. Michael Bubser , Jon R. Backstrom , Elaine Sanders-Bush, Bryan L. Roth and Ariel Y. Deutch. Distribution of Serotonin 5-HT2a Receptors in Afferents of the Rat Striatum, Synapse, 39: 297-304, 2001. 115. T Nguyen, DA Shapiro, SR George, V Setola, DK Lee, R Cheng, L Rauser, SP Lee, KR Lynch, BL Roth and BF O’Dowd: Discovery of a novel member of the histamine receptor family. Mol Pharmacol, 59: 427-433, 2001. 116. BL Roth, P Ernsberger, S Steinberg, S Rao, L Rauser, J Savage, S Hufesein, MS Berridge and RF Muzic,JR. The in vitro pharmacology of the b-adrenergic receptor pet ligand (S)-Fluorocarazolol reveals high affinity for cloned b-adrenergic receptors and moderate affinity for the human 5-HT1A receptor. Psychopharmacol, 157: 111-114, 2001. 117. JA Gray, D Scheffler, S Hufesein, JL Benovic and BL Roth: Cell type-specific role of endocytosis inhibitors in 5-HT2A receptor desensitization and resensitization reveals an arrestin, GRK2- and GRK5-independent regulation in HEK-293 cells. Mol Pharmacol, 60: 1020-1030, 2001.

118. L Rauser, JE Savage, HY Meltzer and BL Roth: Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine2C receptor. J Pharmacol Exp Thera, 299: 83-89, 2001.

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119. Y Huang, LS Kegeles, S Bae, D Hwang, BL Roth, JE Savage and M Laruelle: Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands. Bioorg Med Chem Lett 11: 1375-1377, 2001.

120. R Martin-Ruiz, MV Puig, P Celada, DA Shapiro, BL Roth, G Mengod, F Artigas: Control of serotonergic function in medial prefrontal cortex by serotonin-2A receptors through a glutamate-dependent mechanism. J Neurosci 21: 9856-9866, 2001.

121. BL Roth and DA Shapiro: Insights into the structure and function of 5-HT2-family receptors (5-HT2A, 5-HT2B, 5-HT2C) reveal novel strategies for therapeutic target development. Expert Opinion on Therapeutic Targets. 5: 685-696, 2001.

122. JA Gray and BL Roth: Paradoxical trafficking and regulation of 5-HT2A receptors by agonists and antagonists. Brain Res Bull (Invited Review) 56: 441-451, 2001.

123. C Nocjar, BL Roth and EA Pehek: Colocalization of 5-HT2A receptors on dopamine cells in subnuclei of the midbrain A10 cell group. Neurosci 111: 163-176, 2002.

124. DA Shapiro, KR Kristiansen, DA Weiner, WK Kroeze and BL Roth: Evidence for a model of agonist-induced activation of 5-HT2A serotonin receptors which involves the disruption of a strong ionic interaction between helices 3 and 6. J. Biol. Chem. published January 18, 2002 as 10.1074/jbc.M111675200; 277: 11441-11449, 2002.

125. SP Runyon, S Peddi, JE Savage, BL Roth, RA Glennon and RB Westkaemper. Geometry-affinity relationships of the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene. J Med Chem 45: 1656-1664, 2002.

126. WK Kroeze, K Kristiansen and BL Roth: Molecular biology of serotonin receptors: structure and function at the molecular level. Curr Top Med Chem 2: 507-528, 2002.

127. V Cornea-Hebert, KC Watkins, BL Roth, WK Kroeze, P Gaudreau, N Leclerc, L Descarries: Similar ultrastructural distribution of 5-HT(2A) serotonin receptor and microtubule-associated protein MAP1A in cortical dendrites of adult rat. Neurosci 113: 23-35, 2002.

128. V Butterweck, A Nahrstedt, J Evans, S Hufeisen, L Rauser, J Savage, B Popadak, P Ernsberger and BL Roth: In vitro receptor screening of pure constituents of St. John’s wort reveals novel interactions with a number of GPCRs. Psychopharmacol 162: 193-202, 2002.

129. JA Gray and BL Roth: A last GASP for GPCRs? Science, 297: 529-531, 2002 130. BL Roth, K Baner, RB Westkaemper, KC Rice, S Steinberg, P Ernsberger, and RB Rothman: Salvinorin A: a potent, naturally occurring, non-nitrogenous k-opioid selective agonist. Proc Natl Acad Sci USA, 99: 11934-11939, 2002.

131. AI Faden, SM Knoblach, I Cernak, L Fan, R Vink, GL Araldi, ST Fricke, BL Roth, and AP Kozikowski: Novel diketopiperazine enhances motor and cognitive recovery after traumatic brain injury in rats and shows neuroprotection in vitro and in vivo. J Cereb Blood Flow Metab, 23: 342-354, 2003.

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132. Q Shi, J Savage, S Hufesein, L Rauser, E Grajkowski, P Ernsberger, J Wroblewski, J Nadeau and BL Roth: L-homocysteine sulfinic acid and other acidic homocysteine derivatives are selective metabotropic glutamate receptor agonists. J Pharm Exp Thera 305: 131-142, 2003.

133. DJ Sheffler and BL Roth: Salvinorin A: the ‘magic mint’ hallucinogen finds a molecular target in the kappa opioid receptor. Trends Pharmacol Sci 24:107-109, 2003.

134. WK Kroeze, SJ Hufesein, BA Popadak, SM Renock, S Steinberg, P Ernsberger, K jayathilake, HY Meltzer and BL Roth: H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacol 28: 519-526, 2003

135. Z Xia, JA Gray, BA Compton-Toth and BL Roth: A direct interaction of PSD-95 with the 5-HT2A serotonin receptor regulates signal transduction and receptor trafficking. J Biol Chem 10.1074/jbc.M301905200.

136. JA Gray, A Bhatnagar, VV Guerevich and BL Roth: The interaction of a constitutively active arrestin with the arrestin-insensitive 5-HT2A receptor induces agonist-independent internalization. Mol Pharmacol 63: 961-972, 2003.

137. V Setola, SJ Hufesein, KJ Grande-Allen, I Vesely, RA Glennon, B Blough, RB Rothman, and BL Roth: 3,4-Methylenedioxymethamphetamine (MDMA, "Ecstasy") Induces Fenfluramine-Like Proliferative Actions on Human Cardiac Valvular Interstitial Cells in Vitro. Mol Pharmacol. 63:1223-1229, 2003.

138. DA Shapiro, S Renock, S Arrington, L Chiodo, LX Liu, DR Sibley, BL Roth and RB Mailman: Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology, Neuropsychopharmacol 2003 May 21 [epub ahead of print]; 28: 1400-1411, 2003.

139. S Peddi, BL Roth, RA Glennon and RB Westkaemper: Ring substituted analogues of 5-aminomethyl-10,11-dihydro-dibenzo[a,d]cycloheptene (AMDH): potential modes of binding to the 5-HT(2A) receptor. Bioorg Med Chem Lett 13: 2565-2568, 2003.

140. MS Goldberg, SM Fleming, JJ Palacino, C Cepeda, HA Lam, A Bhatnagar, EG Meloni, N Wu, LC Ackerson, GJ Klapstein, M Gajendiran, BL Roth, MF Chesselet, NT Maidment, MS Levin and J Shen: Parkin-deficient mice exhibit nigrostriatal deficits but not loss of dopaminergic neurons. J Biol Chem 2003 Aug 20 [Epub ahead of print]

141. WK Kroeze, SJ Hufesein, BA Popadak, SM Renock, S Steinberg, P Ernsberger, K Jayathilake, HY Meltzer and BL Roth: Reply to Andrew J Goudie et al Reply: H1 histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacol 2003 Aug 27 [Epub ahead of print]

142. JA Gray, BA Compton-Toth and BL Roth: Identification of two serine residues essential for agonist-induced 5-HT2A receptor desensitization. Biochemistry; [Epub ahead of print] 21-Aug-2003; 42: 10853-10862, 2003.

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143. RB Rothman, N Vu, JS Partilla, BL Roth, SJ Hufeisen, BA Compton-Toth, J Birkes, R Young and RA Glennon: In vitro characterization of epehedrine-related stereoisomers at biogenic amine transporters and the receptorome reveals selective actions as norepinephrine transporter substrates. J Pharmacol Exp Ther 2003 Sep 3 [Epub ahead of print].

144. M DeAmici, P Conti, E Fasoli, E Barocelli, V Ballabeni, S Bertoni, M Impicciatore, BL Roth, P Ernsberger and C De Micheli: Synthesis and in vitro pharmacology of novel hetereocyclic muscarinic ligands. Farmaco 58: 739-748, 2003.

145. BL Roth, D Sheffler and SG Potkin: Atypical antipsychotic drug actions: unitary or multiple mechanisms for ‘atypicality’? Clin Neurosci Res 3: 108-117, 2003.

146. MR Pullagurla, M Dukat, V Setola, B Roth and RA Glennon: N1-benzenesulfonylgramine and N1-benzenesulfonylskatole: novel 5-HT6 receptor templates. Bioorg Med Chem Lett 13: 3355-3359, 2003.

147. WK Kroeze, D Sheffler and BL Roth: G-protein coupled receptors at a glance. J Cell Sci 116: 4867-4869, 2003.

148. X Zia, SJ Hufesein, JA Gray and BL Roth: The PDZ-binding domain is essential for the dendritic targeting of 5-HT(2A) serotonin receptors in cortical pyramidal neurons in vitro. Neurosci 122: 907-920, 2003.

149. V Setola and BL Roth: Why Mice Are Neither Miniature Humans nor Small Rats: A Cautionary Tale Involving 5-Hydroxytryptamine-6 Serotonin Receptor Species Variants.Mol Pharmacol. 64(6):1277-8, 2003.

150. BL Roth, SM Hanizavareh, and AE Blum: Serotonin receptors represent highly favorable molecular targets for cognitive enhancement in schizophrenia and other disorders. Psychopharmacology (Berl). 2003 Dec 2 [Epub ahead of print]

151. S Peddi, BL Roth, RA Glennon and RB Westkaemper: Spiro[9,10-dihydroanthracene]-9,3’-pyrrolidine—a structurally unique tetracyclic 5-HT(2A) receptor antagonist. Eur J Pharmacol 482: 335-337, 2003.

152. BL Roth: Probing the ‘receptorome’ unveils the receptor pharmacology of atypical antipsychotic drugs (in press).

153. Q Shi, SJ Hufeisen, JT Wroblewski, JH Nadeau and BL Roth: L-Homocysteine sulfinic acid and L-homocysteic acid stimulate phosphoinositide hydrolysis in rat cortical neurons. Ann N Y Acad Sci. 1003:461-463, 2003.

154. Chavkin C, Sud S, Jin W, Steward J, Zjawiony JK, Siebert D, Toth BA, Hufeisen SJ, Roth BL.Salvinorin A, an Active Component of the Hallucinogenic Sage Salvia divinorum, is a Highly Efficacious Kappa Opioid Receptor Agonist: Structural and Functional Considerations. J Pharmacol Exp Ther. Mar;308(3):1197-1203. Jan 8 [Epub ahead of print], 2004.

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155. O’Sullivan GJ, BL Roth, A Kinsella, JA Waddington: SK&F 83822 distinguishes adenylyl cyclase from phospholipase C-coupled dopamine D1-like receptors: behavioural topography. Eur J Pharmacol. ;486(3):273-80, 2004.

156. BL Roth, DJ Sheffler and WK Kroeze: Magic shotguns versus magic bullets: why selectively non-selective drugs are superior for drug discovery for mood disorders and schizophrenia. Nature Rev Drug Discovery, 3: 353-359, 2004.

157. JE Piletz, W Deleersnijder, BL Roth, P Ernsberger, H Zhu and D Ziegler: IRAS splice variants. Ann N Y Acad Sci. 1009:419-26, 2003.

158. J Chang-Fong, JB Rangisetty, M Dukat, V Setola, T Raffay, B Roth and RA Glennon: 1,2,3,4-Tetrahydrocarbazoles as 5-HT(6) serotonin receptor ligands. Bioorg Med Chem Lett. 14(8):1961-1964, 2004.

159. S Peddi, BL Roth, RA Glennon and RB Westkaemper: Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(‘)-pyrrolidine (SpAMDA). Bioorg Med Chem Lett 14: 2279-2283, 2004.

160. KA Petri, M Bubser, CD Casey, MD Davis, BL Roth and AY Deutch: The neurotensin agonist PD149163 increases fos expression in the prefrontal cortex of the rat. Neuropsychopharmacol 2004 May 19 [Epub ahead of print].

161. BL Roth, E Lopez, S Beischel, RB Westkaemper, JM Evans: Screening the receptorome to discover the molecular targets for plant-derived psychoactive compounds: a novel approach for CNS drug discovery. Pharmacol Ther 102: 99-110, 2004.

162. A Bhatnagar, DJ Sheffler, WK Kroeze, B Compton-Toth and BL Roth: Caveolin-1 interacts with 5-HT2A serotonin receptors and profoundly modulates the signaling of selected Gaq-coupled GPCRs. J Biol Chem. 2004 Aug 13;279(33):34614-23.

163. PL Quirk, S Rao, BL Roth and RE Siegel: Three putatie N-glycosylation sites within the murine 5-HT3A receptor sequence affect plasma membrane targeting, ligand binding and calcium influx in heterologous mammalian cells. J Neurosci Res 77:498-506, 2004.

164. F Yan and BL Roth: Salvinorin A: a novel and highly selective kappa-opioid receptor agonist. Life Sci 75: 2615-2619,2004 (review).

165. MA Davies, BA Compton-Toth, SJ Hufeisen, HY Meltzer and BL Roth: The highly efficacious actions of N-desmethylclozapine at muscarinic receptors are unique and not a common property of either typical or atypical antipsychotic drugs: is M(1) agonism a pre-requisite for mimicking clozapine's actions? Psychopharmacology (Berl). 2004 Oct 13 [Epub ahead of print]

166. DM Sikazwe, S Li, L Mardenborough, V Cody, BL Roth and SY Ablordeppy: Haloperidol: towards further understanding of the structural contributions of its pharmacophoric elements at D2-like receptors. Bioorg Med Chem Lett. 2004 Dec 6;14(23):5739-42.

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167. GF Elphick; W Querbes, JA Jordan, GV Gee, S Eash, K Manley, A Dugan, M Stanifer, A Bhatnagar, WK Kroeze, BL Roth and WJ Atwood: The human polyoma virus, JCV, uses serotonin receptors to infect cells. Science 306: 1380-1383, 2004.

168. B Karolewicz, K Szebeni, CA Stockmeier, L Konick, JC Overholser, G Jurjus, BL Roth and GA Ordway: Low nNOS protein in the locus coeruleus in major depression. J Neurochem 91: 1057-1066, 2004.

169. BN Armbruster and BL Roth: Mining the receptorome. J Biol Chem 2004 Dec 8 [epub ahead of date].

170. MA Davies, DJ Sheffler, and BL Roth: Aripiprazole: a novel antipsychotic with a uniquely robust pharmacology. CNS Drug Rev 10: 317-336, 2004.

171. BL Roth, WK Kroeze and DJ Sheffler: Fast dissociation rates predict neither efficacy nor lack of side-effects. Nature Rev Drug Discovery, On-line publication 1 Oct 2004 doi: 10.1038/nrd1346-c2.

172. TA Munro, MA Rizzacasa, BL Roth, BA Toth and F Yan: Studies toward the pharmacophore of salvinorin A, a potent kappa opioid receptor agonist. J Med Chem 48: 345-348, 2005

173. D Alagille, RM Baldwin, BL Roth, JT Wroblewski, E Grajkowska, and GD Tamagnan: Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP. Bioorg Med Chem Lett 15: 945-949, 2005

174. D Alagille, RM Baldwin, BL Roth, JT Wroblewski, E Grajkowska and GD Tamangan: Synthesis and receptor assay of aromatic-ethynyl-aromatic derivatives with potent mGluR5 antagonist activity. Bioorg Med Chem 13: 197-209, 2005

175. MS Goldberg, A Pisani, M Haburcak, TA Vortherms, T Kitada, C Costa, Y Tong, G Martella, A Tscherter, A Martins, G Bernardi, BL Roth, EN Pothos, P Calabresi and J Shen: Nigrostriatal dopaminergic deficits and hypokinesia caused by inactivation of the familial parkinsonism-linked gene DJ-1. Neuron published online Feb 3 2005.

176. M Lee, JB Rangisetty, MR Pullagurla, M Duka, V Setola, BL Roth and RA Glennon: 1-(1-napthyl)piperazine as a novel template for 5-HT(6) serotonin receptor ligands. Bioorg Med Chem Lett 15: 1707-1711, 2005.

177. RB Rothman, BE Blough, WL Woolverton, KG Anderson, SS Negus, NK Mello, BL Roth, and MH Baumann: Development of a rationally-designed, low abuse potential, biogenic amine releaser that suppresses cocaine self-administration. J Pharmacol Exp Thera Mar 10 2005 [Epub ahead of print]

178. MA Davies, BA Compton-Toth, SJ Hufeisen, HY Meltzer and BL Roth: The highly efficacious actions of N-desmethylclozapine are unique and not a common property of either typical or atypical antipsychotic drugs: is M(1) agonism a pre-requisite for mimicking clozapine’s actions? Psychpharmacol 178: 451-460 [Epub 2004 Oct 13] 2005.

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179. Y Huang, SA Bae, Z Zhu, N Guo, BL Roth and M Laruelle: Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents. J Med Chem 48: 2559-2570, 2005.

180. R Kolanos, U Siripurapu, M Pellagurla, M Riaz, V Setola, BL Roth, M Dukat, and RA Glennon: Binding of isotryptamines and indenes at h5-HT(6) serotonin receptors. Bioorg Med Chem Lett 15: 1987-1991, 2005.

181. BL Roth and X Zia: Molecular and cellular mechanisms for the polarized sorting of serotonin receptors: relevance for genesis and treatment of psychosis. Crit Rev Neurobiol. 2004;16(4):229-36.

182. VE Setola, M Dukat, RA Glennon and BL Roth: Molecular determinants for the interaction of the valvulopathic anorexigen norfenfluramine with the 5-HT2B receptor. Mol Pharmacol 2005 Apr 14; [Epub ahead of print].

183. TA Vortherms and BL Roth: Receptorome screening for CNS drug discovery. IDrugs 8: 491-496, 2005.

184. F Yan, PD Mosier, RB Westkaemper, J Stewart, JK Zjawiony, TA Vortherms, DJ Sheffler and BL Roth: Identification of the molecular mechanisms by which the diterpenoid salvinorin A binds to kappa-opioid receptors. Biochemistry 44: 8643-8651, 2005.

185. C. Abate, R Kolanos, M Dukat, V Setola, BL Roth and RA Glennon: Interaction of chiral MS-245 analogues at h5-HT(6) receptors. Bioorg Med Chem Lett 2005 Jun 27; [Epub ahead of print].

186. EA Pehek, C Nocjar, BL Roth, TA Byrd and OS Mabrouk: Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the medial prefrontal cortex. Neuropsychopharmacol 2005 Jul 6; [Epub ahead of print].

187. H Sard, G Kumaran, C Morency, BL Roth, BA Toth, P He and L Shuster. SAR of psilocybin analogs: discovery of a selective 5-HT(2C) agonist. Bioorg Med Chem Lett 2005 Jul 29 [epub ahead of print].

188. BL Roth: Receptor systems: will mining the receptorome yield novel targets for pharmacotherapy? Pharmacol Ther 2005 Aug 2 [epub ahead of print].

189. Y Huang, SA Bae, BL Roth and M Laruelle: Synthesis of potent and selective serotonin 5-HT(1B) receptor ligands. Bioorg Med Chem Lett 15: 4786-4789, 2005.

190. AB Beeler, DE Acquilano,Q Su, F Yan, BL Roth, JS Panek and JA Porco: Synthesis of a library of complex macrolides employing cyclodimerization of hydroxyl esters. J Comb Chem 7: 673-781, 2005.

191. M Pullagurla, U Siripurapu, R Kolanos, ML Bondarev, M Dukat, V Setola, BL Roth and RA Glennon: Binding of amine-substituted N(1)-benzensulfonylindoles at human 5-HT(6) serotonin receptors. Bioorg Med Chem Lett [epub ahead of print].

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192. O’Connor KA and BL Roth: Screening the receptorome for plant-based psychoactive compounds. Life Sci [Oct 4 2005 epub ahead of print. 193. Sondergaard K, Kristensen JL, Palner M, Gillings N, Knudsen GM, Roth BL, Begtrup M.

Synthesis and binding studies of 2-arylapormorphines. Org Biomol Chem 3: 4077-4081, 2005.

194. Munro TA, GW Goetchius, BL Roth, TA Vortherms and MA Rizzacasa. Autoxidation of

salvinorin A under basic conditions.J Org Chem. 2005 Nov 25;70(24):10057-61. 195. Davies MA, V Setola, RT Strachen, DJ Sheffler, E Salay, SJ Hufeisen, and BL Roth:

Pharmacologic analysis of non-synonymous conding h5-HT(2A) SNP’s reveals alterations in atypical antipsychotic and agonist efficacies. Pharmacogenomics J 2005 Nov 29 [Epub ahead of print].

196. O’Connor KA and BL Roth: Finding new tricks for old drugs: an efficient route for public

sector drug discovery. Nature Rev Drug Discov 4: 1005-1014, 2005. 197. Kushwaha N, SC Harwood, AM Wilson, M Berger, LH Tecott, BL Roth and PR Albert:

Molecular determinants in the second intracellular loop of the 5-hydroxytrypamine(1A)(5-HT1A) receptor for G-protein coupling. Mol Pharmacol 2006 Jan 27 [Epub ahead of date].

198. Iso Y, E Grajkowska, JT Wroblewski, J Davis, NE Goeders, KM Johnson, S Sanker, BL

Roth, W Tueckmantel and AP Kozikowski: Synthesis and structure-activity relationships of 3[(2-Methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonsits; search for cocaine medications. J Med Chem 49: 1080-1100, 2006.

199. Ablordeppey SY, Lyles-Eggleston M, Bricker B, Zhang W, Zhu X, Goodman C, Roth

BL.Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol.Bioorg Med Chem Lett. 2006 Apr 16; [Epub ahead of print]

200. DJ Sheffler, WK Kroeze, SJ Hufesein, P Lehey, BG Garcia, AY Deutch, J Bruning and BL

Roth: p90 ribosomal S6 kinase exerts a ‘tonic brake’ on G protein coupled receptor signaling. Proc Natl Acad Sci USA, 103(12):4717-22, 2006.

201. DJ Stewart, H Fahmy, BL Roth, F Yan andJK Zjawiony: Bioisoteric modification of

salvinorin A, a potent and selective kappa-opioid receptor agonist. Arzeim-Forsch./Drug Res 56: 289-275, 2006.

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202. WK Kroeze and BL Roth: Screening the receptorome. J Psychopharmacol. 2006 Jul;20(4 Suppl):41-6.

203. Urban JD, Clarke WP, von Zastrow M, Nichols DE, Kobilka BK, Weinstein H, Javitch JA,

Roth BL, Christopoulos A, Sexton P, Miller K, Spedding M, Mailman RB. Functional selectivity and classical concepts of quantitative pharmacology. J Pharmacol Exp Ther. 2006 Jun 27; [Epub ahead of print]

204. Strachan RT, Ferrara G, Roth BL. Screening the receptorome: an efficient approach for

drug discovery and target validation. Drug Discov Today. 2006 Aug;11(15-16):708-16. Review.

205. V Setola and BL Roth: Screening the receptorome reveals molecular targets responsible

for drug-induced side effects: focus on 'fen-phen'. Expert Opin Drug Metab Toxicol. 2005 Oct;1(3):377-87. Review.

206. Sikazwe D, Bondarev ML, Dukat M, Rangisetty JB, Roth BL, Glennon RA. Binding of

sulfonyl-containing arylalkylamines at human 5-HT6 serotonin receptors. J Med Chem. 2006 Aug 24;49(17):5217-25.

207. Chemel BR, Roth BL, Armbruster B, Watts VJ, Nichols DE. WAY-100635 is a potent

dopamine D(4) receptor agonist. Psychopharmacology (Berl). 2006 Oct;188(2):244-51. Epub 2006 Aug 17.

UNIVERSITY OF NORTH CAROLINA CHAPEL HILL MEDICAL SCHOOL PUBLICATIONS 208. Kolanos R, Dukat M, Roth BL, Glennon RA. Interaction of N(1)-unsubstituted and N(1)-

benzenesulfonyltryptamines at h5-HT(6) receptors. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5832-5835. Epub 2006 Aug 30.

209. AP Kozikowski, B Roth and A Tropsha: Why academic drug discovery makes sense.

Science 313: 1235-1236, 2006. 210. TA Vortherms and BL Roth: Salvinorin A: from natural product to human therapeutics. Mol

Interventions 6: 257-65, 2006 {Cover} 211. Dandapani S, Lan P, Beeler AB, Beischel S, Abbas A, Roth BL, Porco JA Jr, Panek JS.:

Convergent Synthesis of Complex Diketopiperazines Derived from Pipecolic Acid Scaffolds and Parallel Screening against GPCR Targets. J Org Chem. 2006 Nov 10;71(23):8934-8945.

212. Roth BL: Contributions of molecular biology to antipsychotic drug discovery: promises

fulfilled or unfulfilled? Dialogues Clin Neurosci. 2006;8(3):303-9. 213. Vortherms TA, Mosier PD, Westkaemper RB, Roth BL. Differential helical orientations

among related G protein-coupled receptors provide a novel mechanism for selectivity: Studies with salvinorin A and the kappa opioid receptor. J Biol Chem. 2006 Nov 22; [Epub ahead of print]

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214. Roth, BL: Drugs and valvular heart disease. N Engl J Med. 2007;356(1):6-9 (BLR interviewed by NY Times, Wall Street Journal, CNN, MSNBC, NPR All Things Considered and many other media outlets)

215. Keiser MJ, Roth BL, Armbruster BN, Ernsberger P, Irwin JJ, Shoichet BK. Relating protein

pharmacology by ligand chemistry. Nature Biotechnol. 2007 Feb;25(2):197-206. 216. BN Armbruster, X Li, S Herlitzer, M Pausch and BL Roth: Evolving the

lock to fit the key to create a family of GPCRs potently activated by an inert ligand. Proc Natl Acad Sci 2007 Mar 20;104(12):5163-8.

217. JA Gray and BL Roth: Molecular Targets for Treating Cognitive Dysfunction in Schizophrenia. Schizophr Bull. 2007 Jul 7; [Epub ahead of print]

218. JA Gray and BL Roth: The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Jul 31; [Epub ahead of print]

219. Dallanoce C, De Amici M, Barocelli E, Bertoni S, Roth BL, Ernsberger P, De Micheli C.Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes. Bioorg Med Chem. 2007 Dec 15;15(24):7626-37. Epub 2007 Sep 11.

220. Beguin C, Potter DN, Dinieri JA, Munro TA, Richards MR, Paine TA, Berry L, Zhao Z, Roth BL, Xu W N-methylacetamide analogue of salvinorin A: a highly potent and selective kappa opioid receptor agonist with oral efficacy.J Pharmacol Exp Ther. 2007 Oct 19.

221. Roth, BL: Dopamine agonists and valvular heart disease. N Engl J Med 356: 1676-1680, 2007.

222. Carato P, Graulich A, Jensen N, Roth BL, Liégeois JF. Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part I: Influence of the substitution on the basic nitrogen and the position of the amide on the affinity for D2L, D4.2, and 5-HT2A receptors.Bioorg Med Chem Lett. 2007 Mar 15;17(6):1565-9. Epub 2007 Jan 8

223. Carato P, Graulich A, Jensen N, Roth BL, Liégeois JF. Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part II: Influence of the substitution on the benzyl moiety on the affinity for D2L, D4.2, and 5-HT2A receptors.Bioorg Med Chem Lett. 2007 Mar 15;17(6):1570-4. Epub 2007 Jan 8

224. Jensen NH, Rodriguiz RM, Caron MG, Wetsel WC, Rothman RB, Roth BL. N-Desalkylquetiapine, a Potent Norepinephrine Reuptake Inhibitor and Partial 5-HT(1A) Agonist, as a Putative Mediator of Quetiapine's Antidepressant Activity.Neuropsychopharmacology. 2007 Dec 5; [Epub ahead of print]

225. Svenningsson P, Bateup H, Qi H, Takamiya K, Huganir RL, Spedding M, Roth BL, McEwen BS, Greengard P. Involvement of AMPA receptor phosphorylation in antidepressant actions with special reference to tianeptine .Eur J Neurosci. 2007 Dec;26(12):3509-17.

226. Abbas A and Roth BL: Arresting serotonin. Proc Natl Acad Sci USA 105: 831-832, 2008. 227. Dukat M, Mosier PD, Kolanos R, Roth BL, Glennon RA. Binding of serotonin and N1-

benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies.J Med Chem. 2008 Feb 14;51(3):603-11. Epub 2008 Jan 18.

228. Yan F, Mosier PD, Westkaemper RB, Roth BL. Galpha-subunits differentially alter the conformation and agonist affinity of kappa-opioid receptors. Biochemistry. 2008 Feb 12;47(6):1567-78.

229. Conn PJ and Roth BL: The challenges and opportunities of psychiatric drug discovery: roles for scientists in academic, industry and government settings. Neuropsychopharmacol 2008 Jan 23 [epub ahead of print]

230. Roth BL: High dose olanzapine for treatment resistant schizophrenia. J Clin Psych 69: 176-177, 2008.

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231. Wald DN, Vermaat HM, Zang S, Lavik A, Kang Z, Peleg G, Gerson SL, Bunting KD, Agarwal ML, Roth BL, Tse W. Identification of 6-benzylthioinosine as a myeloid leukemia differentiation-inducing compound. Cancer Res. 2008 Jun 1;68(11):4369-76.

232. Ablordeppey SY, Altundas R, Bricker B, Zhu XY, Suresh Kumar EV, Jackson T, Khan A, Roth BL. Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-Chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. Bioorg Med Chem. 2008 Jun 20. [Epub ahead of print]

233. Nawaratne V, Leach K, Suratman N, Loiacono RE, Felder CC, Armbruster BN, Roth BL, Sexton PM, Christopoulos A. New insights into the function of M4 muscarinic acetylcholine receptors gained using a novel allosteric modulator and a "designer receptor exclusively activated by a designer drug" (DREADD).Mol Pharmacol. 2008 Jul 15. [Epub ahead of print]

234. Allan JA, P Yadov and BL Roth: Insights into the regulation of 5-HT(2A) receptors by scaffolding proteins and kinases. .Neuropharmacology. 2008 Jul 2. [Epub ahead of print]

235. Conklin BR, Hsiao EC, Claeysen S, Dumuis A, Srinivasan S, Forsayeth JR, Guettier JM, Chang WC, Pei Y, McCarthy KD, Nissenson RA, Wess J, Bockaert J, Roth BL. Engineering GPCR signaling pathways with RASSLs. Nature Methods. 2008 Aug;5(8):673-8.

236. Jensen NH and Roth BL: Massively parallel screening of the receptorome. Comb Chem High Throughput Screen 11: 420-426, 2008.

237. Basura GJ, Abbas AI, O’Donohue H, Lauder JM, Roth BL, Walker PD and Manis PB: Ontogeny of serotonin and serotonin(2A) receptors in rat auditory cortex. Hear Res 2008 Aug 6 [epub ahead of print]

238. Dewkar GK, Peddi S, Mosier PD, Roth BL and Westkaemper RB: Methoxy-substituted 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives exhibit differential binding affinities at the 5-HT(2A) receptor.Bioorg Med Chem Lett. 2008 Aug 22. [Epub ahead of print]

239. Han D, Holger Försterling F, Li X, Deschamps JR, Parrish D, Cao H, Rallapalli S, Clayton T, Teng Y, Majumder S, Sankar S, Roth BL, Sieghart W, Furtmuller R, Rowlett JK, Weed MR, Cook JM. A study of the structure-activity relationship of GABA(A)-benzodiazepine receptor bivalent ligands by conformational analysis with low temperature NMR and X-ray analysis.Bioorg Med Chem. 2008 Oct 1;16(19):8853-62. Epub 2008 Sep 2.

240. Ma ZZ, Xu W, Jensen NH, Roth BL, Liu-Chen LY, Lee DY. Isoquinoline alkaloids isolated from Corydalis yanhusuo and their binding affinities at the dopamine D1 receptor.Molecules. 2008 Sep 25;13(9):2303-12.

241. Abbas, A and Roth BL: Protein engineering: electrifying receptors. Nature Nanotechnology, 3: 587-588, 2008

242. Runyon SP, Mosier PD, Roth BL, Glennon RA, Westkaemper RB. Potential Modes of Interaction of 9-Aminomethyl-9,10-dihydroanthracene (AMDA) Derivatives with the 5-HT2A Receptor: A Ligand Structure-Affinity Relationship, Receptor Mutagenesis and Receptor Modeling Investigation.J Med Chem. 2008 Oct 11. [Epub ahead of print]

243. Abbas, A and Roth BL: Pimavanserin tartrate: a 5-HT2A inverse agonist with potential for treating various neuropsychiatric disorders. Expert Opinion Pharmacother. 9: 3251-3259, 2008.

244. Pei Y, Rogan SC, Yan F and Roth BL: Engineered GPCRs as tools to modulate signal transduction. Physiology 23: 313-321, 2008.

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245. Strachan RT, Sheffler DJ, Willard B, Kinter M, Kiselar JG, Roth BL. Ribosomal S6 Kinase 2 Directly Phosphorylates the 5-Hydroxytryptamine 2A (5-HT2A) Serotonin Receptor, Thereby Modulating 5-HT2A Signaling. J Biol Chem. 2009 Feb 27;284(9):5557-73. Epub 2008 Dec 22.

246. Sikazwe DM, Nkansah NT, Altundas R, Zhu XY, Roth BL, Setola V, Ablordeppey SY. Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups. Bioorg Med Chem. 2009 Feb 15;17(4):1716-23. Epub 2008 Dec 31.

247. Tang H, Wang XS, Huang XP, Roth BL, Butler KV, Kozikowski AP, Jung M, Tropsha A.Novel Inhibitors of Human Histone Deacetylase (HDAC) Identified by QSAR Modeling of Known Inhibitors, Virtual Screening, and Experimental Validation. Bioorg Med Chem. 2009 Feb 15;17(4):1716-23. Epub 2008 Dec 31.

248. Zolkowska D, Jain R, Rothman RB, Partilla JS, Roth BL, Setola V, Prisinzano TE and Bauman MH: Evidence for the involvement of dopamine transporters in behavioral stimulant effects of modafanil. J Pharm Exp Thera 2009 Feb 5 [epub ahead of print]

249. Bibukbulatov RV, Stewart J, Jin W, Yan F, Roth BL, Ferreira D, Zjawiony JK. Short synthesis of a novle class of salvinorin A analogues with hemiacetalic structure. Tetrahedron Lett 49: 937-940, 2008.

250. Rivas FM, Stables JP, Murphree L, Edwankar RV, Edwankar CR, Huang S, Jain HD, Zhou H, Majumder S, Sankar S, Roth BL, Ramerstorfer J, Furtmüller R, Sieghart W, Cook JM. Antiseizure Activity of Novel gamma-Aminobutyric Acid (A) Receptor Subtype-Selective Benzodiazepine Analogues in Mice and Rat Models. J Med Chem 2009 Mar 10 [epub ahead of print]

251. Cho SJ, Jensen NH, Kurome T, Kadari S, Manzano ML, Malberg JE, Caldarone B, Roth BL, Kozikowski AP. Selective 5-Hydroxytryptamine 2C Receptor Agonists Derived from the Lead Compound Tranylcypromine: Identification of Drugs with Antidepressant-Like Action. J Med Chem 2009 March 13 [epub ahead of print]

252. Abbas AI, Hedlund PB, Huang XP, Tran TB, Meltzer HY, Roth BL. Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo. Psychopharmacology (Berl). 2009 Jul;205(1):119-28.

253. Abbas AI, Yadav PN, Yao WD, Arbuckle MI, Grant SG, Caron MG, Roth BL. PSD-95 is essential for hallucinogen and atypical antipsychotic drug actions at serotonin receptors. J Neurosci. 2009 Jun 3;29(22):7124-36

254. Alexander GM, Rogan SC, Abbas AI, Armbruster BN, Pei Y, Allen JA, Nonneman RJ, Hartmann J, Moy SS, Nicolelis MA, McNamara JO, Roth BL. Remote control of neuronal activity in transgenic mice expressing evolved G protein-coupled receptors. Neuron. 2009 Jul 16;63(1):27-39.

255. Guettier JM, Gautam D, Scarselli M, Ruiz de Azua I, Li JH, Rosemond E, Ma X, Gonzalez FJ, Armbruster BN, Lu H, Roth BL, Wess J. A chemical-genetic approach to study G protein regulation of beta cell function in vivo. Proc Natl Acad Sci U S A. 2009 Nov 10;106(45):19197-202.

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256. Huang XP, Setola V, Yadav PN, Allen JA, Rogan SC, Hanson BJ, Revankar C, Robers M, Doucette C, Roth BL. Parallel functional activity profiling reveals valvulopathogens are potent 5-hydroxytryptamine(2B) receptor agonists: implications for drug safety assessment. Mol Pharmacol. 2009 Oct;76(4):710-22.

257. Hwang JY, Arnold LA, Zhu F, Kosinski A, Mangano TJ, Setola V, Roth BL, Guy RK. Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors. J Med Chem. 2009 Jul 9;52(13):3892-901.

258. Jones KA, Srivastava DP, Allen JA, Strachan RT, Roth BL, Penzes P. Rapid modulation of spine morphology by the 5-HT2A serotonin receptor through kalirin-7 signaling. Proc Natl Acad Sci U S A. 2009 Nov 17;106(46):19575-80.

259. Keiser MJ, Setola V, Irwin JJ, Laggner C, Abbas AI, Hufeisen SJ, Jensen NH, Kuijer MB, Matos RC, Tran TB, Whaley R, Glennon RA, Hert J, Thomas KL, Edwards DD, Shoichet BK, Roth BL. Predicting new molecular targets for known drugs. Nature. 2009 Nov 12;462(7270):175-81 (Faculty of 1000; Highlighted in Nature, Science, Nature Reviews Drug Discovery and listed as one of Top 10 Scientific Achievements of 2009 by Wired Magazine, among others).

260. Kimple AJ, Soundararajan M, Hutsell SQ, Roos AK, Urban DJ, Setola V, Temple BR, Roth BL, Knapp S, Willard FS, Siderovski DP. Structural determinants of G-protein alpha subunit selectivity by regulator of G-protein signaling 2(RGS2). J Biol Chem. 2009 May 28.

261. Nichols CD, Roth BL. Engineered G-protein Coupled Receptors are Powerful Tools to Investigate Biological Processes and Behaviors. Front Mol Neurosci. 2009;2:16.

262. Rivas FM, Stables JP, Murphree L, Edwankar RV, Edwankar CR, Huang S, Jain HD, Zhou H, Majumder S, Sankar S, Roth BL, Ramerstorfer J, Furtmuller R, Sieghart W, Cook JM. Antiseizure Activity of Novel gamma-Aminobutyric Acid (A) Receptor Subtype-Selective Benzodiazepine Analogues in Mice and Rat Models. J Med Chem. 2009 Mar 10.

263. Shah JR, Mosier PD, Roth BL, Kellogg GE, Westkaemper RB. Synthesis, structure-affinity relationships, and modeling of AMDA analogs at 5-HT2A and H1 receptors: structural factors contributing to selectivity. Bioorg Med Chem. 2009 Sep 15;17(18):6496-504.

264. Strachan RT, Sciaky N, Cronan MR, Kroeze WK, Roth BL. Genetic deletion of p90 ribosomal S6 kinase 2 alters patterns of 5-HT2A serotonin receptor functional selectivity. Mol Pharmacol. 2009 Nov 20.

265. Strachan RT, Sheffler DJ, Willard B, Kinter M, Kiselar JG, Roth BL. Ribosomal S6 Kinase 2 Directly Phosphorylates the 5-Hydroxytryptamine 2A (5-HT2A) Serotonin Receptor, Thereby Modulating 5-HT2A Signaling. J Biol Chem. 2009 Feb 27;284(9):5557-73.

266. Yan F, Bikbulatov RV, Mocanu V, Dicheva N, Parker CE, Wetsel WC, Mosier PD, Westkaemper RB, Allen JA, Zjawiony JK, Roth BL. Structure-based design, synthesis, and biochemical and pharmacological characterization of novel salvinorin A analogues as active state probes of the kappa-opioid receptor. Biochemistry. 2009 Jul 28;48(29):6898-908.

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267. Abbas, A.I., Urban, D.J., Jensen, N.H., Farrell, M.S., Kroeze, W.K., Mieczkowski, P., Wang, Z., and Roth, B.L. Assessing serotonin receptor mRNA editing frequency by a novel ultra high-throughput sequencing method. Nucleic Acids Res 2010, 38, e118.

268. Davies, M.A., Conley, Y., and Roth, B.L. Functional SNPs in Genes Encoding the 5-HT2A Receptor Modify the Affinity and Potency of Several Atypical Antipsychotic Drugs. Biol Res Nurs.

269. Dong, S., Allen, J.A., Farrell, M., and Roth, B.L. A chemical-genetic approach for precise spatio-temporal control of cellular signaling. Mol Biosyst.

270. Dong, S., Rogan, S.C., and Roth, B.L. Directed molecular evolution of DREADDs: a generic approach to creating next-generation RASSLs. Nature Protocols 2010, 5, 561-573.

271. Farrell, M., and Roth, B.L. Allosteric antipsychotics: m4 muscarinic potentiators as novel treatments for schizophrenia. Neuropsychopharmacology , 2010, 35, 851-852.

272. Glennon, R.A., Siripurapu, U., Roth, B.L., Kolanos, R., Bondarev, M.L., Sikazwe, D., Lee, M., and Dukat, M. The medicinal chemistry of 5-HT6 receptor ligands with a focus on arylsulfonyltryptamine analogs. Curr Top Med Chem 2010, 10, 579-595.

273. Magalhaes, A.C., Holmes, K.D., Dale, L.B., Comps-Agrar, L., Lee, D., Yadav, P.N.,

Drysdale, L., Poulter, M.O., Roth, B.L., Pin, J.P., et al. CRF receptor 1 regulates anxiety behavior via sensitization of 5-HT2 receptor signaling. Nat Neurosci 2010, 13, 622-629.

274. McGovern, D.L., Mosier, P.D., Roth, B.L., and Westkaemper, R.B. CoMFA analyses of C-2

position Salvinorin A analogs at the kappa-opioid receptor provides insights into epimer selectivity. J Mol Graph Model 2010, 28, 612-625.

275. Morabito, M.V., Abbas, A.I., Hood, J.L., Kesterson, R.A., Jacobs, M.M., Kump, D.S.,

Hachey, D.L., Roth, B.L., and Emeson, R.B. Mice with altered serotonin 2C receptor RNA editing display characteristics of Prader-Willi syndrome. Neurobiol Dis I2010, 39, 169-180.

276. Nemeth, C.L., Paine, T.A., Rittiner, J.E., Beguin, C., Carroll, F.I., Roth, B.L., Cohen, B.M.,

and Carlezon, W.A., Jr. Role of kappa-opioid receptors in the effects of salvinorin A and ketamine on attention in rats. Psychopharmacology (Berl) 2010, 210, 263-274.

277. Pei, Y., Dong, S., and Roth, B.L. Generation of designer receptors exclusively activated by

designer drugs (DREADDs) using directed molecular evolution. Curr Protoc Neurosci Chapter 4, Unit 4 33, 2010.

278. Savic, M.M., Majumder, S., Huang, S., Edwankar, R.V., Furtmuller, R., Joksimovic, S.,

Clayton, T., Sr., Ramerstorfer, J., Milinkovic, M.M., Roth, B.L., et al. Novel positive allosteric modulators of GABAA receptors: do subtle differences in activity at alpha1 plus alpha5 versus alpha2 plus alpha3 subunits account for dissimilarities in behavioral effects in rats? Prog Neuropsychopharmacol Biol Psychiatry 34, 376-386, 2010.

279. Shah, J.R., Mosier, P.D., Peddi, S., Roth, B.L., and Westkaemper, R.B. 9-Aminomethyl-9,10-dihydroanthracene (AMDA) analogs as structural probes for steric tolerance in 5-HT2A and H1 receptor binding sites. Bioorg Med Chem Lett 20, 935-938, 2010.

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280. Strachan, R.T., Allen, J.A., Sheffler, D.J., and Roth, B.L. p90 Ribosomal S6 kinase 2, a novel GPCR kinase, is required for growth factor-mediated attenuation of GPCR signaling. Biochemistry 49, 2657-2671, 2010.

281. Strachan, R.T., Sciaky, N., Cronan, M.R., Kroeze, W.K., and Roth, B.L. Genetic deletion of

p90 ribosomal S6 kinase 2 alters patterns of 5-hydroxytryptamine 2A serotonin receptor functional selectivity. Mol Pharmacol 77, 327-338, 2010.

282. Allen JA, Roth BL. Strategies to Discover Unexpected Targets for Drugs Active at G

Protein-Coupled Receptors. Annu Rev Pharmacol Toxicol. Jan 18 2011 283. Ferguson SM, Eskenazi D, Ishikawa M, Wanat MJ, Phillips PE, Dong Y, et al. Transient

neuronal inhibition reveals opposing roles of indirect and direct pathways in sensitization. Nat Neurosci. Jan;14(1):22-4, 2011

284. Fichna J, Lewellyn K, Yan F, Roth BL, Zjawiony JK. Synthesis and biological evaluation of

new salvinorin A analogues incorporating natural amino acids. Bioorg Med Chem Lett. Jan 1;21(1):160-3, 2011.

285. Frankowski KJ, Ghosh P, Setola V, Tran TB, Roth BL, Aube J. N-Alkyl-

octahydroisoquinolin-1-one-8-carboxamides: a Novel Class of Selective, Nonbasic, Nitrogen-Containing kappa-Opioid Receptor Ligands. ACS Med Chem Lett. Aug 12;1(5):189-93, 2010

286. Frankowski KJ, Setola V, Evans JM, Neuenswander B, Roth BL, Aube J. Organic

Synthesis Toward Small-Molecule Probes and Drugs Special Feature: Synthesis and receptor profiling of Stemona alkaloid analogues reveal a potent class of sigma ligands. Proc Natl Acad Sci U S A. Feb 28, 2011

287. Hajjo R, Grulke CM, Golbraikh A, Setola V, Huang XP, Roth BL, et al. Development,

validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs. J Med Chem. Nov 11;53(21):7573-86, 2010

288. Huang XP, Mangano T, Hufeisen S, Setola V, Roth BL. Identification of Human Ether-a-go-

go Related Gene Modulators by Three Screening Platforms in an Academic Drug-Discovery Setting. Assay Drug Dev Technol. Dec;8(6):727-42, 2010

289. Kozikowski AP, Cho SJ, Jensen NH, Allen JA, Svennebring AM, Roth BL. HTS and rational drug design to generate a class of 5-HT(2C)-selective ligands for possible use in schizophrenia. ChemMedChem. Aug 2;5(8):1221-5, 2010.

290. Kwon YJ, Saubern S, Macdonald JM, Huang XP, Setola V, Roth BL. N-

tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B. Bioorg Med Chem Lett. Sep 15;20(18):5488-90, 2010

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291. McKenna DJ, Ruiz JM, Hoye TR, Roth BL, Shoemaker AT. Receptor screening technologies in the evaluation of Amazonian ethnomedicines with potential applications to cognitive deficits. J Ethnopharmacol. Mar 24;134(2):475-92, 2011

292. Oury F, Sumara G, Sumara O, Ferron M, Chang H, Smith CE, et al. Endocrine regulation

of male fertility by the skeleton. Cell. Mar 4;144(5):796-809, 2011

293. Rogan SC, Roth BL. Remote Control of Neuronal Signaling. Pharmacol Rev. Mar 17, 2011

294. Roth BL. Irving page lecture 5-HT(2A) serotonin receptor biology: Interacting proteins,

kinases and paradoxical regulation. Neuropharmacology. Feb 1, 2011 295. Yadav PN, Abbas AI, Farrell MS, Setola V, Sciaky N, Huang XP, et al. The Presynaptic

Component of the Serotonergic System is Required for Clozapine's Efficacy. Neuropsychopharmacology. Nov 3, 2010

296. Hutcheson JD, Setola V, Roth BL, Merryman WD., Serotonin receptors and heart valve

disease—it was meant 2B. Pharmacol Thera 2011 Mar 23 [epub ahead of print] 297. Yin W, Majumder S, Clayton T, Petrou S, VanLinn ML, Namjoshi OA, Ma C, Cromer BA,

Roth BL, Platt DM, Cook JM. Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse. Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.

298. Krashes MJ, Koda S, Ye C, Rogan SC, Adams AC, Cusher DS, Maratos-Flier E, Roth BL,

Lowell BB. Rapid, reversible activation of AgRP neurons drives feeding behavior in mice. J Clin Invest. 2011 Mar 1. pii: 46229. doi: 10.1172/JCI46229

299. Allen JA, Yost JM, Setola V, Chen X, Sassano MF, Chen M, Peterson S, Yadav PN, Huang

XP, Feng B, Jensen NH, Che X, Bai X, Frye SV, Wetsel WC, Caron MG, Javitch JA, Roth BL and Jin J Discovery of beta-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy. Proc Natl Acad Sci U S A 108:18488-18493

(BLR and JJ Co-Corresponding Authors)

300. Carlsson J, Coleman RG, Setola V, Irwin JJ, Fan H, Schlessinger A, Sali A, Roth BL and

Shoichet BK Ligand discovery from a dopamine D3 receptor homology model and crystal structure. Nature Chem Biol 7:769-778. (BLR and BKS Co-Corresponding Authors)

301. Gupta K, Chakrabarti A, Rana S, Ramdeo R, Roth BL, Agarwal ML, Tse W, Agarwal MK

and Wald DN Securinine, a myeloid differentiation agent with therapeutic potential for AML. PLoS One 6:e21203.

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302. Laggner C, Kokel D, Setola V, Tolia A, Lin H, Irwin JJ, Keiser MJ, Cheung CY, Minor DL, Jr., Roth BL, Peterson RT and Shoichet BK Chemical informatics and target identification in a zebrafish phenotypic screen. Nature Chem Biol. 2011 Dec 18. doi: 10.1038/nchembio.732. [Epub ahead of print]

(BLR, RTP and BKS Co-Corresponding Authors) 303. Vardy E and Roth BL Vision and olfaction say UNC-le to G proteins. Nature Neurosci

14:805-806.

304. Vedadi M, Barsyte-Lovejoy D, Liu F, Rival-Gervier S, Allali-Hassani A, Labrie V, Wigle TJ, Dimaggio PA, Wasney GA, Siarheyeva A, Dong A, Tempel W, Wang SC, Chen X, Chau I, Mangano TJ, Huang XP, Simpson CD, Pattenden SG, Norris JL, Kireev DB, Tripathy A, Edwards A, Roth BL, Janzen WP, Garcia BA, Petronis A, Ellis J, Brown PJ, Frye SV, Arrowsmith CH and Jin J A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nature Chem Biol 7:566-574.

305. Yadav PN, Kroeze WK, Farrell MS and Roth BL Antagonist functional selectivity: 5-HT2A

serotonin receptor antagonists differentially regulate 5-HT2A receptor protein level in vivo. J Pharmacol Exp Ther 339:99-105.

306. Huang, H-S, Allen JA, Mabb AM, King IF, Miriyala J, Taylor B, Sciaky N, Dutton JW, Lee H-

M, Chen X, Jin J, Bridges AS, Zylka MJ, Roth BL and Philpot BD. Topoisomerase inhibitors unsilence the dormant allele of Ube3A in neurons. Nature, doi:10.1038/nature10726

(BLR, MJZ and BDP Co-Corresponding Authors) 307. Chen X, Sassano MF, Zheng L, Setola V, Chen M, Bai X, Frye SV, Wetsel WC, Roth BL

and Jin J (2012) Structure-Functional Selectivity Relationship Studies of beta-Arrestin-Biased Dopamine D(2) Receptor Agonists. J Med Chem 55:7141-7153.

(BLR and JJ Co-Corresponding Authors) 308. Garner AR, Rowland DC, Hwang SY, Baumgaertel K, Roth BL, Kentros C and Mayford M

(2012) Generation of a synthetic memory trace. Science 335:1513-1516. 309. Gregori-Puigjane E, Setola V, Hert J, Crews BA, Irwin JJ, Lounkine E, Marnett L, Roth BL

and Shoichet BK (2012) Identifying mechanism-of-action targets for drugs and probes. Proc Natl Acad Sci U S A 109:11178-11183.

(BLR and BKS Co-Correspoding Authors) 310. Hajjo R, Setola V, Roth BL and Tropsha A (2012) A Chemocentric Informatics Approach to

Drug Discovery: Identification and Experimental Validation of Selective Estrogen Receptor Modulators as ligands of 5-Hydroxytryptamine-6 Receptors and as Potential Cognition Enhancers. J Med Chem.

311. Thompson AA, Liu W, Chun E, Katritch V, Wu H, Vardy E, Huang XP, Trapella C, Guerrini R, Calo G, Roth BL, Cherezov V and Stevens RC (2012) Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic. Nature 485:395-399.

312. Wu H, Wacker D, Mileni M, Katritch V, Han GW, Vardy E, Liu W, Thompson AA, Huang XP, Carroll FI, Mascarella SW, Westkaemper RB, Mosier PD, Roth BL, Cherezov V and

46

Stevens RC (2012) Structure of the human kappa-opioid receptor in complex with JDTic. Nature.

313. Farrell, M.S., Pei, Y., Wan, Y., Yadav, P.N., Daigle, T.L., Urban, D.J., Lee, H.M., Sciaky, N., Simmons, A., Nonneman, R.J., et al. A Galpha(s) DREADD Mouse for Selective Modulation of cAMP Production in Striatopallidal Neurons. Neuropsychopharmacology, in press

314. Farrell, M.S., and Roth, B.L. Pharmacosynthetics: Reimagining the pharmacogenetic approach. Brain Res., in press

315. Fischer, B.D., Licata, S.C., Edwankar, R.V., Wang, Z.J., Huang, S., He, X., Yu, J., Zhou, H., Johnson, E.M., Jr., Cook, J.M., et al. Anxiolytic-like effects of 8-acetylene imidazobenzodiazepines in a rhesus monkey conflict procedure. Neuropharmacology 59, 612-618.

316. Gupta, K., Chakrabarti, A., Rana, S., Ramdeo, R., Roth, B.L., Agarwal, M.L., Tse, W., Agarwal, M.K., and Wald, D.N. Securinine, a myeloid differentiation agent with therapeutic potential for AML. PLoS One 6, e21203.

317. Hajjo, R., Grulke, C.M., Golbraikh, A., Setola, V., Huang, X.P., Roth, B.L., and Tropsha, A. Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs. J Med Chem 53, 7573-7586 2012.

318. Iversen, L., Gibbons, S., Treble, R., Setola, V., Huang, X.P., and Roth, B.L. Neurochemical profiles of some novel psychoactive substances. Eur J Pharmacol., in press

319. Lee, H.M., and Roth, B.L. Hallucinogen actions on human brain revealed. Proc Natl Acad Sci U S A 109, 1820-1821, 2012.

320. Li, J., Fronczek, F.R., Ferreira, D., Burandt, C.L., Jr., Setola, V., Roth, B.L., and Zjawiony, J.K. Bis-spirolabdane diterpenoids from Leonotis nepetaefolia. J Nat Prod 75, 728-734, 2012.

321. Lin, X., Huang, X.P., Chen, G., Whaley, R., Peng, S., Wang, Y., Zhang, G., Wang, S.X., Wang, S., Roth, B.L., et al. Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors. J Med Chem 55, 5749-5759, 2012.

322. Namjoshi, O.A., Wang, Z.J., Rallapalli, S.K., Johnson, E.M., Jr., Johnson, Y.T., Ng, H., Ramerstorfer, J., Varagic, Z., Sieghart, W., Majumder, S., et al. Search for alpha3beta(2/3)gamma2 subtype selective ligands that are stable on human liver microsomes. Bioorg Med Chem 21, 93-101, 2012

323. Roth, B.L., and Marshall, F.H. NOBEL 2012 Chemistry: Studies of a ubiquitous receptor family. Nature 492, 57, 2012

324. Twiner, M.J., Doucette, G.J., Rasky, A., Huang, X.P., Roth, B.L., and Sanguinetti, M.C. Marine algal toxin azaspiracid is an open-state blocker of hERG potassium channels. Chem Res Toxicol 25, 1975-1984, 2012

325. White, K.L., and Roth, B.L. Psychotomimetic effects of kappa opioid receptor agonists. Biol Psychiatry 72, 797-798, 2012

326. Wu, H., Li, J., Fronczek, F.R., Ferreira, D., Burandt, C.L., Jr., Setola, V., Roth, B.L., and Zjawiony, J.K. Labdane Diterpenoids from Leonotis leonurus. Phytochemistry, in press

327. Zhu, H., Urban, D.J., Blashka, J., McPheeters, M.T., Kroeze, W.K., Mieczkowski, P., Overholser, J.C., Jurjus, G.J., Dieter, L., Mahajan, G.J., et al. Quantitative analysis of focused a-to-I RNA editing sites by ultra-high-throughput sequencing in psychiatric disorders. PLoS One 7, e43227, 2012.

328. Agulhon C, Boyt KM, Xie AX, Friocourt F, Roth BL, McCarthy KD. 2013. Modulation of the autonomic nervous system and behaviour by acute glial cell Gq protein-coupled receptor activation in vivo. J Physiol 591: 5599-609

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329. Arunotayanun W, Dalley JW, Huang XP, Setola V, Treble R, et al. 2013. An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'. Bioorg Med Chem Lett 23: 3411-5

330. Becnel J, Johnson O, Majeed ZR, Tran V, Yu B, et al. 2013. DREADDs in Drosophila: a pharmacogenetic approach for controlling behavior, neuronal signaling, and physiology in the fly. Cell Rep 4: 1049-59

331. Carroll FI, Gichinga MG, Williams JD, Vardy E, Roth BL, et al. 2013. 4beta-Methyl-5-(3-hydroxyphenyl)morphan Opioid Agonist and Partial Agonist Derived from a 4beta-Methyl-5-(3-hydroxyphenyl)morphan Pure Antagonist. J Med Chem 56: 8826-33

332. Farrell MS, Pei Y, Wan Y, Yadav PN, Daigle TL, et al. 2013. A Galphas DREADD mouse for selective modulation of cAMP production in striatopallidal neurons. Neuropsychopharmacology 38: 854-62

333. Farrell MS, Roth BL. 2013. Pharmacosynthetics: Reimagining the pharmacogenetic approach. Brain Res 1511: 6-20

334. Ferguson SM, Phillips PE, Roth BL, Wess J, Neumaier JF. 2013. Direct-pathway striatal neurons regulate the retention of decision-making strategies. J Neurosci 33: 11668-76

335. Goldsmith JR, Perez-Chanona E, Yadav PN, Whistler J, Roth BL, Jobin C. 2013. Intestinal epithelial cell-derived mu-opioid signaling protects against ischemia reperfusion injury through PI3K signaling. Am J Pathol 182: 776-85

336. Iversen L, Gibbons S, Treble R, Setola V, Huang XP, Roth BL. 2013. Neurochemical profiles of some novel psychoactive substances. Eur J Pharmacol 700: 147-51

337. Kim J, Kim Y, Tae J, Yeom M, Moon B, et al. 2013. Aryl Biphenyl-3-ylmethylpiperazines as 5-HT Receptor Antagonists. ChemMedChem

338. Kim Y, Kim J, Tae J, Roth BL, Rhim H, et al. 2013. Discovery of aryl-biphenyl-2-ylmethylpiperazines as novel scaffolds for 5-HT(7) ligands and role of the aromatic substituents in binding to the target receptor. Bioorg Med Chem 21: 2568-76

339. Kokel D, Cheung CY, Mills R, Coutinho-Budd J, Huang L, et al. 2013. Photochemical activation of TRPA1 channels in neurons and animals. Nature Chem Biol

340. Konze KD, Ma A, Li F, Barsyte-Lovejoy D, Parton T, et al. 2013. An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol 8: 1324-34

341. Lee HM, Giguere PM, Roth BL. 2013. DREADDs: novel tools for drug discovery and development. Drug Discov Today

342. Lemieux GA, Keiser MJ, Sassano MF, Laggner C, Mayer F, et al. 2013. In silico molecular comparisons of C. elegans and mammalian pharmacology identify distinct targets that regulate feeding. PLoS Biol 11: e1001712

343. Lin H, Sassano MF, Roth BL, Shoichet BK. 2013. A pharmacological organization of G protein-coupled receptors. Nature Methods 10: 140-6

344. Liu F, Barsyte-Lovejoy D, Li F, Xiong Y, Korboukh V, et al. 2013. Discovery of an in Vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP. J Med Chem 56: 8931-42

345. Liu R, Huang XP, Yeliseev A, Xi J, Roth BL. 2013. Novel Molecular Targets of Dezocine and Their Clinical Implications. Anesthesiology

346. Matsunaga F, Gao L, Huang XP, Saven JG, Roth BL, Liu R. 2013. Molecular interactions between general anesthetics and the 5HT receptor. J Biomol Struct Dyn

347. McElligott ZA, Fox ME, Walsh PL, Urban DJ, Ferrel MS, et al. 2013. Noradrenergic synaptic function in the bed nucleus of the stria terminalis varies in animal models of anxiety and addiction. Neuropsychopharmacology 38: 1665-73

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348. Meltzer HY, Roth BL. 2013. Lorcaserin and pimavanserin: emerging selectivity of serotonin receptor subtype-targeted drugs. J Clin Invest 123: 4986-91

349. Munro TA, Huang XP, Inglese C, Perrone MG, Van't Veer A, et al. 2013. Selective kappa opioid antagonists nor-BNI, GNTI and JDTic have low affinities for non-opioid receptors and transporters. PLoS One 8: e70701

350. Namjoshi OA, Wang ZJ, Rallapalli SK, Johnson EM, Jr., Johnson YT, et al. 2013. Search for alpha3beta(2)/(3)gamma2 subtype selective ligands that are stable on human liver microsomes. Bioorg Med Chem 21: 93-101

351. Parnaudeau S, O'Neill PK, Bolkan SS, Ward RD, Abbas AI, et al. 2013. Inhibition of mediodorsal thalamus disrupts thalamofrontal connectivity and cognition. Neuron 77: 1151-62

352. Polepally PR, White K, Vardy E, Roth BL, Ferreira D, Zjawiony JK. 2013. Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands. Bioorg Med Chem Lett

353. Riss PJ, Hong YT, Marton J, Caprioli D, Williamson DJ, et al. 2013. Synthesis and evaluation of 18F-FE-PEO in rodents: an 18F-labeled full agonist for opioid receptor imaging. J Nucl Med 54: 299-305

354. Roth BL. 2013. Impossible or merely difficult? Two grand challenges from a biologist's perspective. ACS Med Chem Lett 4: 316-18

355. Roth BL, Gibbons S, Arunotayanun W, Huang XP, Setola V, et al. 2013. The ketamine analogue methoxetamine and 3- and 4-methoxy analogues of phencyclidine are high affinity and selective ligands for the glutamate NMDA receptor. PLoS One 8: e59334

356. Sassano MF, Doak A, Roth BL, Shoichet BK. 2013. Colloidal Aggregation Causes Inhibition of G Protein-Coupled Receptors. J Med Chem

357. Vardy E, Mosier PD, Frankowski KJ, Wu H, Katritch V, et al. 2013. Chemotype-selective modes of action of kappa-opioid receptor agonists. J Biol Chem 288: 34470-83

358. Vardy E, Roth BL. 2013. Conformational ensembles in GPCR activation. Cell 152: 385-6 359. Wacker D, Wang C, Katritch V, Han GW, Huang XP, et al. 2013. Structural features for

functional selectivity at serotonin receptors. Science 340: 615-9 360. Wang C, Jiang Y, Ma J, Wu H, Wacker D, et al. 2013. Structural basis for molecular

recognition at serotonin receptors. Science 340: 610-4 361. Wang C, Wu H, Katritch V, Han GW, Huang XP, et al. 2013. Structure of the human

smoothened receptor bound to an antitumour agent. Nature 362. Weiss DR, Ahn S, Sassano MF, Kleist A, Zhu X, et al. 2013. Conformation guides

molecular efficacy in docking screens of activated beta-2 adrenergic G protein coupled receptor. ACS Chem Biol 8: 1018-26

363. Wu H, Li J, Fronczek FR, Ferreira D, Burandt CL, Jr., et al. 2013. Labdane diterpenoids from Leonotis leonurus. Phytochemistry 91: 229-35

364. Yin W, Majumder S, Clayton T, Petrou S, VanLinn ML, et al. 2013. Design, synthesis, and subtype selectivity of 3,6-disubstituted beta-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse. Bioorg Med Chem 18: 7548-64

365. Fenalti G, Giguere PM, Katritch V, Huang XP, Thompson AA, Cherezov V, Roth BL and Stevens RC 2014. Molecular control of delta-opioid receptor signaling. Nature 506(7487):191-6

366. Fourches D, Sassano MF, Roth BL, Tropsha A. 2014. HTS navigator: freely accessible cheminformatics software for analyzing high-throughput screening data. Bioinformatics

367. Giguere PM, Kroeze WK, Roth BL. 2014. Tuning up the right signal: chemical and genetic approaches to study GPCR functions. Curr Opin Cell Biol 27: 51-55

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368. Luo M, Wang XS, Roth BL, Golbraikh A, Tropsha A. 2014. Application of Quantitative Structure-Activity Relationship Models of 5-HT1A Receptor Binding to Virtual Screening Identifies Novel and Potent 5-HT1A Ligands. J Chem Inf Model

369. White KL, Scopton AP, Rives ML, Bikbulatov RV, Polepally PR, Brown PJ, Kenakin T, Javitch JA, Zjawiony, JK and Roth BL 2014. Identification of novel functionally selective kappa-opioid receptor scaffolds. Mol Pharmacol 85: 83-90

370. Jin C, Decker AM, Huang XP, Gilmour BP, Blough BE, Roth BL, Hu Y, Gill JB and Zhang XP 2014. Synthesis, Pharmacological Characterization, and Structure-Activity Relationship Studies of Small Molecular Agonists for the Orphan GPR88 Receptor. ACS Chem Neurosci 5:576-87

371. Katritch V, Fenalti G, Abola EE, Roth BL, Cherezov V, Stevens RC. 2014. Allosteric sodium in class A GPCR signaling. Trends Biochem Sci 39:233-44

372. Lee HM, Giguere PM, Roth BL. 2014. DREADDs: novel tools for drug discovery and development. Drug Discov Today 19:469-73

373. Liu R, Huang XP, Yeliseev A, Xi J, Roth BL. 2014. Novel molecular targets of dezocine and their clinical implications. Anesthesiology 120:714-23

374. Luo M, Wang XS, Roth BL, Golbraikh A, Tropsha A. 2014. Application of quantitative structure-activity relationship models of 5-HT1A receptor binding to virtual screening identifies novel and potent 5-HT1A ligands. J Chem Inf Model 54:634-47

375. Obradovic A, Joksimovic S, Poe MM, Ramerstorfer J, Varagic Z, Namjoshi, O.Batinic, B.Radulovic, T.,Markovic, B., Roth, B.L., Sieghart, W.,Cook, J. M., Savic, M. M. 2014. Sh-I-048A, an in vitro non-selective super-agonist at the benzodiazepine site of GABAA receptors: the approximated activation of receptor subtypes may explain behavioral effects. Brain Res 1554:36-48

376. Sampson D, Bricker B, Zhu XY, Peprah K, Lamango NS, Setola V, Roth BL and Ablordeppy SY 2014a. Further evaluation of the tropane analogs of haloperidol. Bioorg Med Chem Lett

377. Sampson D, Zhu XY, Eyunni SV, Etukala JR, Ofori E, Bricker B, Lamango SN, Setola V, Roth BL and Ablordeppy SY 2014b. Identification of a new selective dopamine D4 receptor ligand. Bioorg Med Chem 22:3105-14

378. Sternson SM, Roth BL. 2014. Chemogenetic tools to interrogate brain functions. Annu Rev Neurosci 37:387-407

379. Wang C, Wu H, Evron T, Vardy E, Han GW, Huang XP, Mangano TJ, Urban DJ, Katrich, V, Cherezov V, Caron MG, Roth BL and Stevens RC 2014. Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs. Nature Commun 5:4355

380. Zhu H, Pleil KE, Urban DJ, Moy SS, Kash TL, Roth BL. 2014. Chemogenetic inactivation of ventral hippocampal glutamatergic neurons disrupts consolidation of contextual fear memory. Neuropsychopharmacology 39:1880-92

381. Zhu H, Roth BL. 2014. Silencing synapses with DREADDs. Neuron 82:723-5

382. Polepally PR, Huben K, Vardy E, Setola V, Mosier PD, Roth BL, Zjawiony JK. Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor. Eur J Med Chem. 2014 Oct 6;85:818-29.

383. Urban DJ and Roth BL: DREADDs: chemogenetic tools with therapeutic utility. Ann Rev Pharmacol 2014 Sep 25. [Epub ahead of print]

384. White KL, Robinson JE, Zhu H, DiBerto JF, Polepally PR, Zjawiony JK, Nichols DE, Malanga CJ, Roth BL. The G Protein-Biased κ-Opioid Receptor Agonist RB-64 Is Analgesic

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with a Unique Spectrum of Activities In Vivo. J Pharmacol Exp Ther. 2015 Jan;352(1):98-109.

385. Cero C, Vostrikov VV, Verardi R, Severini C, Gopinath T, Braun PD, Sassano MF, Gurney A, Roth BL, Vulchanova L, Possenti R, Veglia G, Bartolomucci A. The TLQP-21 Peptide Activates the G-Protein-Coupled Receptor C3aR1 via a Folding-upon-Binding Mechanism. Structure. 2014 Dec 2;22(12):1744-53.

386. Zhu, H and Roth BL. DREADD: a chemogenetic signaling platform. Int J Neuropsychopharmacol 2014 Oc 31. pii:pyu007 [epub ahead of print].

387. Chen X, Choo H, Huang XP, Yang X, Stone O, Roth BL, Jin J. The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs. ACS Chem Neurosci. 2015 Mar 18;6(3):476-84

388. McCorvy JD and Roth BL: Structure and function of serotonin receptors. Pharmacol Thera 2015 Jan 17. pii: S0163-7258(15)00029-7. doi: 10.1016/j.pharmthera.2015.01.009. [Epub ahead of print]

389. Cheng J, Giguère PM, Onajole OK, Lv W, Gaisin A, Gunosewoyo H, Schmerberg CM, Pogorelov VM, Rodriguiz RM, Vistoli G, Wetsel WC, Roth BL, Kozikowski AP. Optimization of 2-phenylcyclopropylmethlamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. J Med Chem 26: 1992-2002, 201

390. Fenalti G, Zatsepin NA, Betti C, Giguere P, Han GW, Ishchenko A, Liu W, Guillemyn K, Zhang H, James D, Wang D, Weierstall U, Spence JC, Boutet S, Messerschmidt M, Williams GJ, Gati C, Yefanov OM, White TA, Oberthuer D, Metz M, Yoon CH, Barty A, Chapman HN, Basu S, Coe J, Conrad CE, Fromme R, Fromme P, Tourwé D, Schiller PW, Roth BL, Ballet S, Katritch V, Stevens RC, Cherezov V. Structural basis for bifuntional peptide recognition at human d-opioid receptor. Nature Struc Mol Biol 22: 265-268, 2015

391. Kaniskan HÜ, Szewczyk MM, Yu Z, Eram MS, Yang X, Schmidt K, Luo X, Dai M, He F,

Zang I, Lin Y, Kennedy S, Li F, Dobrovetsky E, Dong A, Smil D, Min SJ, Landon M, Lin-Jones J, Huang XP, Roth BL, Schapira M, Atadja P, Barsyte-Lovejoy D, Arrowsmith CH, Brown PJ, Zhao K, Jin J, Vedadi M. A potent, selective and cell-active allosteric inhibitor of protein argininine methyltransferase 3 (PRMT3). Agnew Chem Int Ed Engl 2015 Feb 27. doi: 10.1002/anie.201412154. [Epub ahead of print]

392. Nocjar C, Alex KD, Sonneborn A, Abbas A, Roth BL and Pehek EA. Serotonin-2C and 2a

receptor co-expression on cells in the rat medial prefrontal cortex. Nueroscience 2015 Mar 27. pii: S0306-4522(15)00287-0. doi: 10.1016/j.neuroscience.2015.03.050. [Epub ahead of print]

393. Elliott Robinson J, Vardy E, DiBerto JF, Chefer VI, White KL, Fish EW, Chen M, Gigante E,

Krouse MC, Sun H, Thorsell A, Roth BL, Heilig M, Malanga CJ. Receptor Reserve Moderates Mesolimbic Responses to Opioids in a Humanized Mouse Model of the OPRM1 A118G Polymorphism. Neuropsychopharmacology. 2015 Apr 16. doi: 10.1038/npp.2015.109. [Epub ahead of print]

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394. Kroeze WK, Sassano MF, Huang XP, Lansu K, McCorvy JD, Giguère PM, Sciaky N, Roth

BL. PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome. Nature Struct Mol Biol. 22: 362-369, 2015.

395. Vardy E, Robinson JE, Li C, Olsen RH, DiBerto JF, Giguere PM, Sassano FM, Huang XP,

Zhu H, Urban DJ, White KL, Rittiner JE, Crowley NA, Pleil KE, Mazzone CM, Mosier PD, Song J, Kash TL, Malanga CJ, Krashes MJ, Roth BL.A New DREADD facilitates the multiplexed chemogenetic interrogation of behavior. Neuron, 86: 936-46, 2015.

396. Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE,

Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Roth B, Ross R, Schapira M, Schreiber SL,Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ. The promise and peril of chemical probes. Nature Chemical Biol 11: 536-541, 2015.

397. Marchant NJ, Whitaker LR, Bossert JM, Harvey BK, Hope BT, Kaganovsky K, Adhikary S,

Prisinzano TE, Vardy E, Roth BL, Shaham Y. Behavioral and Physiological Effects of a Novel Kappa-Opioid Receptor-Based DREADD in Rats. Neuropsychopharmacology. 2015 May 28.

398. Salaga M, Polepally PR, Zielinska M, Marynowski M, Fabisiak A, Murawska N, Sobczak K,

Sacharczuk M, Do Rego JC, Roth BL, Zjawiony JK, Fichna J. Salvinorin A analogues PR-37 and PR-38 attenuate compound 48/80-induced itch responses in mice. Br J Pharmacol. 2015 Sep;172(17):4331-41.

399. Vardy E, Sassano MF, Rennekamp AJ, Kroeze WK, Mosier PD, Westkaemper RB,

Stevens CW, Katritch V, Stevens RC, Peterson RT, Roth BL. Single Amino Acid Variation Underlies Species-Specific Sensitivity to Amphibian Skin-Derived Opioid-like Peptides Chemistry and Biology 2015 Jun 18;22(6):764-75.

400. Roth BL and Kroeze WK. Integrated Approaches for Genome-wide Interrogation of the

Druggable Non-olfactory G Protein-coupled Receptor Superfamily. J Biol Chem. 2015 Aug 7;290(32):19471-7.

401. Cheng J, Giguere PM, Lv W, Roth BL, Kozikowski AP Design and Synthesis of (2-(5-

Chloro-2,2-dimethyl-2,3-dihydrobenzofuran-7-yl)cyclopropyl)methanamine as a Selective Serotonin 2C Agonist. Tetrahedron Lett. 2015 Jun 3;56(23):3420-3422.

402. Zhang Z, Kil KE, Poutiainen P, Choi JK, Kang HJ, Huang XP, Roth BL, Brownell AL. Re-

exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability. Bioorg Med Chem Lett. 2015 Sep 15;25(18):3956-60.

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403. O'Connor C, White KL, Doncescu N, Didenko T, Roth BL, Czaplicki G, Stevens RC, Wüthrich K, Milon A. NMR structure and dynamics of the agonist dynorphin peptide bound to the human kappa opioid receptor. Proc Natl Acad Sci USA 112: 11852-11857, 2015

404. Urban DJ, Zhu H, Marcinkiewcz CA, Michaelides M, Oshibuchi H, Rhea D, Aryal DK,

Farrell MS, Lowery-Gionta E, Olsen RH, Wetsel WC, Kash TL, Hurd YL, Tecott LH, Roth BL Elucidation of the behavioral program and neuronal network encoded by dorsal raphe serotonergic neurons. Neuropsychopharmacol 2015 Sep 18. doi: 10.1038/npp.2015.293. [Epub ahead of print]

405. English JG and Roth BL: Chemogenetics--A transformational and translational platform. JAMA Neurology Sep 26: 1-6, 2015.

406. Huang XP, Karpiak J, Kroeze WK, Zhu H, Chen X, Moy SS, Saddoris KA, Nikolova VD,

Farrell MS, Wang S, Mangano TJ, Deshpande DA, Jiang A, Penn RB, Jin J, Koller BH, Kenakin T, Shoichet BK, Roth BL . Discovery of allosteric modulators for the pharmacologically dark receptors GPR68 and GPR65. Nature, 527: 477-483, 2015.

407. Cheng J, Giguère PM, Schmerberg CM, Pogorelov VM, Rodriguiz RM, Huang XP, Zhu H,

McCorvy JD, Wetsel WC, Roth BL, Kozikowski AP. Further advances in optimizing (2-phenylcyclopropyl)methylamines as novel serotonin 2C agonists: effects on hyperlocomotion, prepulse inhibition and cognition models. J Med Chem 2015 Dec 24 [epub ahead of date], 59: 578-91, 2016.

408. Elkins JM, Fedele V, Szklarz M, Abdul Azeez KR, Salah E, Mikolajczyk J, Romanov S,

Sepetov N, Huang XP, Roth BL, Al Haj Zen A, Fourches D, Muratov E, Tropsha A, Morris J, Teicher BA, Kunkel M, Polley E, Lackey KE, Atkinson FL, Overington JP, Bamborough P, Müller S, Price DJ, Willson TM, Drewry DH, Knapp S, Zuercher WJ Comprehensive characterizaiton of the published kinase inhibitor set. Nature Biotechnol 2015 Oct 26 [epub ahead of date], 34: 95-103, 2016

409. Stuckey JI, Dickson BM, Cheng N, Liu Y, Norris JL, Cholensky SH, Tempel W, Qin S,

Huber KG, Sagum C, Black K, Li F, Huang XP, Roth BL, Baughman BM, Senisterra G, Pattenden SG, Vedadi M, Brown PJ, Bedford MT, Min J, Arrowsmith CH, James LI, Frye SV. A Cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1. Nature Chemical Biology 12: 180-187, 2016

410. Bruchas MR and Roth BL: New technologies for elucidating opioid receptor function.

Trends Pharmacol Sci 2016 Jan 29. pii: S0165-6147(16)00002-X. doi: 10.1016/j.tips.2016.01.001. [Epub ahead of print]

411. Roth BL: DREADDs for Neuroscientists. Neuron 89: 683-694, 2016

412. Farrell MS, McCorvy JD, Huang XP, Urban DJ, White KL, Giguere PM, Doak AK, Bernstein AI, Stout KA, Park SM, Rodriguiz RM, Gray BW, Hyatt WS, Norwood AP, Webster KA, Gannon BM, Miller GW, Porter JH, Shoichet BK, Fantegrossi WE, Wetsel WC, Roth BL. In

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vitro and in vivo characterization of the alkaloid nuciferine. PLosOne 11(3):e0150602. doi: 10.1371/journal.pone.0150602. eCollection 2016.

413. Wacker D and Roth BL: An alerting structrue: human orexin receptor 1. Nature Structural

and Molecular Biology 23: 265-266, 2016. 414. Etukala JR, Zhu XY, Eyunni SV, Onyameh EK, Ofori E, Bricker BA, Kang HJ, Huang

XP, Roth BL, Ablordeppey SY. Development of CNS multi-receptor ligands: modificaiton of known D2 pharmacophores. Bioorg Med Chem 24: 3671-9, 2016

415. Ofori E, Zhu XY, Etukala JR, Peprah K, Jordan KR, Adkins AA, Bricker BA, Kang HJ,

Huang XP, Roth BL, Ablordeppey SY. Designa nd synthesis of dual 5-HT1A and 5-HT7 receptor ligands. Bioorg Med Chem 24: 3464-71, 2016

416. Grace PM, Strand KA, Galer EL, Urban DJ, Wang X, Baratta MV, Fabisiak TJ, Anderson

ND, Cheng K, Greene LI, Berkelhammer D, Zhang Y, Ellis AL, Yin HH, Campeau S, Rice KC, Roth BL, Maier SF, Watkins LR. Morphine paradoxically prolongs neuropathic pain in rats by amplifying spinal NLRP3 inflammasome activation. Proc Natl Acad Sci USA 113: E3441-50, 2016

417. Rennekamp AJ, Huang XP, Wang Y, Patel S, Lorello PJ, Cade L, Gonzales AP, Yeh JR,

Caldarone BJ,Roth BL, Kokel D, Peterson RT.s1 recetpor ligands control a switch between passive and active threat responses Nature Chemical Biology 12: 552-8, 2016

418. Bruni G, Rennekamp AJ, Velenich A, McCarroll M, Gendelev L, Fertsch E, Taylor J,

Lakhani P, Lensen D, Evron T, Lorello PJ, Huang XP, Kolczewski S, Carey G, Caldarone BJ, Prinssen E, Roth BL, Keiser MJ, Peterson RT, Kokel D. Zebrafish behavioral profiling identifies multitarget antipscychotic-like compounds. Nature Chemical Biology 12: 559-66, 2016

419. Zhu H, Aryal DK, Olsen RH, Urban DJ, Swearingen A, Forbes S, Roth BL,

Hochgeschwender U. Cre-dependent DREADD (Designer Reptor Exclusively Activated by Designer Drug) mice. Genesis 54: 439-46, 2016

420. Chan JD, McCorvy JD, Acharya S, Johns ME, Day TA, Roth BL, Marchant JS. A

mineaturized screen of a Schistosoma mansoni serotonergic G protein-coupled receptor identifies novel classes of parasite-selective inhibitors. PLOS Pathogens 12:e1005651, 2016.

421. Manglik A, Lin H, Aryal DK, McCorvy JD, Dengler D, Corder G, Levit A, Kling RC, Bernat V,

Hübner H, Huang XP, Sassano MF, Giguère PM, Löber S, Da Duan, Scherrer G, *Kobilka BK, *Gmeiner P,* Roth BL, *Shoichet BK. Structure-based discovery of opioid analgesics with reduced side-effects. Nature Aug 17:1-6. doi: 10.1038/nature19112. (*=Corresponding authors)

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422. Cheng, J, McCorvy JD, Giguere PM, Zhu H, Kenakin, T, Roth BL and Kozikowski AP: Design and discovery of functionally selective serotonin2C (5-HT2C) receptor agonists. J Med Chem 10: 9866-9880, 2016

423. Breen G, Li Q, Roth BL, O'Donnell P, Didriksen M, Dolmetsch R, O'Reilly PF, Gaspar HA, Manji H, Huebel C, Kelsoe JR, Malhotra D, Bertolino A, Posthuma D, Sklar P, Kapur S, Sullivan PF, Collier DA, Edenberg HJ. Translating genome-wide association findings into new therapeutics for psychiatry. Nature Neurosci, 19: 1392-1396, 2016

424. Sato, S, Huang XP, Kroeze WK and Roth BL: Discovery and characterization of novel

GPR39 agonists allosterically modulated by zinc. Mol Pharmacol 90: 726-737, 2016 425. McCovy JC, Olsen RH and Roth BL: Psilocybin for depression and anxiety associated with

life-threatening illnesses. J Psychopharmacol 30: 1209-1210, 2016. 426. Urs NM, Gee SM, Pack TF, McCorvy JD, Evron T, Snyder JC, Yang X, Rodriguiz RM,

Borrelli E, Wetsel WC, Jin J, Roth BL, O'Donnell P, Caron MG. Distinct cortical and striatal actions of a b-arresin-biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties. Proc Natl Acad Sci USA 113: E178-E186, 2016.

427. Kim, Y., H.M. Lee, Y. Xiong, N. Sciaky, S.W. Hulbert, X. Cao, J.I. Everitt, J. Jin, B.L. Roth*, and Y.H. Jiang*, Targeting the histone methyltransferase G9a activates imprinted genes and improves survival of a mouse model of Prader-Willi syndrome. Nat Med, 23(2):213-222, 2017 *=Co-corresponding authors

428. Zheng, Z., X.P. Huang, T.J. Mangano, R. Zou, X. Chen, S.A. Zaidi, B.L. Roth, R.C. Stevens, and V. Katritch, Structure-Based Discovery of New Antagonist and Biased Agonist Chemotypes for the Kappa Opioid Receptor. J Med Chem, 60(7): 3070-3081, 2017

429. Le Gonidec, S., C. Chaves-Almagro, Y. Bai, H.J. Kang, A. Smith, E. Wanecq, X.P. Huang, H. Prats, B. Knibiehler, B.L. Roth, L.S. Barak, M.G. Caron, P. Valet, Y. Audigier, and B. Masri, Protamine is an antagonist of apelin receptor, and its activity is reversed by heparin. FASEB J, 31(6): 2507-2519, 2017.

430. Lansu, K., J. Karpiak, J. Liu, X.P. Huang, J.D. McCorvy, W.K. Kroeze, T. Che, H. Nagase, F.I. Carroll, J. Jin, B.K. Shoichet, and B.L. Roth, In silico design of novel probes for the atypical opioid receptor MRGPRX2. Nat Chem Biol, 2017. 13(5): 529-536, 2017

431. Wacker, D., S. Wang, J.D. McCorvy, R.M. Betz, A.J. Venkatakrishnan, A. Levit, K. Lansu, Z.L. Schools, T. Che, D.E. Nichols, B.K. Shoichet, R.O. Dror, and B.L. Roth, Crystal Structure of an LSD-Bound Human Serotonin Receptor. Cell, 2017. 168(3): 377-389, 2017

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432. Pogorelov VM, Rodriguiz RM, Cheng J, Huang M, Schmerberg CM, Meltzer HY, Roth BL, Kozikowski AP, Wetsel WC. 5-HT2C agonists modulate schizophrenia-like behaviors in miceNeuropsychopharmacology. 2017 Apr 12. doi: 10.1038/npp.2017.52. [Epub ahead of print]

433. Zhang G, Cheng J, McCorvy JD, Lorello PJ, Caldarone BJ, Roth BL, Kozikowski AP. Discovery of N-substituted (2-phenylcyclopropyl)methylamines as functionally selective serotonin 2C receptor agonists for potential uses as antipsychotic medications. J Med Chem. 2017 Jul 27;60(14):6273-6288.

434. Ishchenko A, Wacker D, Kapoor M, Zhang A, Han GW, Basu S, Patel N, Messerschmidt M, Weierstall U, Liu W, Katritch V, Roth BL, Stevens RC, Cherezov V. Structural insights into the extracellular recogntion of the human serotonin 2B receptor by an antibody. Proc Natl Acad Sci USA 114: 8223-8228, 2017.

435. Axen SD, Huang XP, Cáceres EL, Gendelev L, Roth BL, Keiser MJ. A simple representation of three-dimensional molecular structure. J Med Chem. 2017 Jul 21. doi: 10.1021/acs.jmedchem.7b00696. [Epub ahead of print]

436. Wacker D, Stevens RC, Roth BL. How ligands illuminate GPCR molecular pharmacology. Cell 170:414-427, 2017.

437. Wang, S, Wacker D, Levit A, Che T, Betz RM, McCorvy JD, Venkatakrishnan AJ, Huang X-

P, Dror RO, Shoichet BK and Roth BL. D4 dopamine receptor high resolution structures tenable the discovery of selective agonists. Science 358: 381-386, 2017

438. Pera T, Deshpande DA, Ippolito M, Wang B, Gavrila A, Michael JV, Nayak AP, Tompkins

E, Farrell E, Kroeze WK, Roth BL, Panettieri RA Jr, Benovic JL, An SS, Dulin NO, Penn RB. Biased signaling of the proton-sensing receptor OGR1 by benzodiazepines. FASEB J2017 Oct 17. pii: fj.201700555R. doi: 10.1096/fj.201700555R. [Epub ahead of print]

439. Roth BL, Irwin JJ and Shoichet BK. Discovery of new GPCR ligands to illuminate new

biology. Nature Chemical Biology 13: 1143-1151, 2017. 440. Che, T, Majumdar S, Zaidi, SA, Ondachi P, McCovry JD, Wang S, Mosier PD, Uprety R,

Vardy E, Krumm BE, Han GW, Lee M-Y, Pardon E, Steyaert J, Huang X-P, Strachan RT, Tribo AR, Pasternak GW,Carroll FI, Stevens RC, Cherezov V, Katritch V, Wacker D and Roth BL: Structure of a nanobody-stabilized active state of the kappa opioid receptor. Cell 172: 55-6, 2018.

441. Huang XP, Che T, Mangano TJ, Le Rouzic V, Pan YX, Cameron MD, Baumann MH, Pasternak GW, Roth BL. Fentanyl-related designer drugs W-18 and W-15 lack appreciable opioid activity in vitro and in vivo. JCI Insight 2017 2:22. pii: 97222

442. Chan JD, Cupit PM, Gunaratne GS, McCorvy JD, Yang Y, Stoltz K, Webb TR, Dosa

PI, Roth BL, Abagyan R, Cunningham C, Marchant JS. The antihelminitic praziquantel is a

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human serotonergic G-protein-coupled receptor iigand. Nature Communications 8: 1910, 2017

443. McCorvy JD, Butler KV, Kelly B, Rechsteiner K, Karpiak J, Betz RM, Kormos BL, Shoichet

BK, Dror RO, Jin J, Roth BL. Structure-inspired design of b-arrestin biased ligands for aminergic GPCRs. Nature Chemical Biology 2017 Dec 11 [epub ahead of print]

444. Wang S, Che T, Levit A, Shoichet BK, Wacker D and Roth BL: Structure of the D2 dopamine receptor bound to the atypical antipsychotic drug risperidone. Nature 555: 269-273, 2018.

445. Pera T, Deshpande DA, Ippolito M, Wang B, Gavrila A, Michael JV, Nayak AP, Tompkins E, Farrell E, Kroeze WK, Roth BL, Panettieri RA Jr., Benovic JL, An SS, Dulin NO, Penn RB. Biased signaling of the proton-sensing recetpor OGR1 by benzodiazepines. FASEB J 32: 862-874, 2018

446. Peng Y, McCorvy JD, Harpsøe K, Lansu K, Yuan S, Popov P, Qu L, Pu M, Che T, Nikolajsen LF, Huang XP, Wu Y, Shen L, Bjørn-Yoshimoto WE, Ding K, Wacker D, Han GW, Cheng J, Katritch V, Jensen AA, Hanson MA, Zhao S, Gloriam DE, Roth BL, Stevens RC, Liu ZJ. 5-HT2C receptor structures reveal the structural basis of GPCR polypharmacology. Cell 172: 719-730, 2018.

447. Gaspar HA, Collier DA, Geschwind DH, Lewis CM, Li Q, Roth BL, Sullivan PF, Breen G. Conference report: Psychiatric Genomics Consortium Meeting: Pathways to Drugs, London, March 2017. Biol Psych in press

448. Oprea TI, Bologa CG, Brunak S, Campbell A, Gan GN, Gaulton A, Gomez SM, Guha R, Hersey A, Holmes J, Jadhav A, Jensen LJ, Johnson GL, Karlson A, Leach AR, Ma'ayan A, Malovannaya A, Mani S, Mathias SL, McManus MT, Meehan TF, von Mering C, Muthas D, Nguyen DT, Overington JP, Papadatos G, Qin J, Reich C, Roth BL, Schürer SC, Simeonov A, Sklar LA, Southall N, Tomita S, Tudose I, Ursu O, Vidovic D, Waller A, Westergaard D, Yang JJ, Zahoránszky-Köhalmi G. Unexplored therapeutic opportunities in the human genome. Nature Rev Drug Discov, in press.

449.

INVITED LECTURES (Partial list; approximate titles listed). 1 Synaptic membrane and smooth microsomal opiate receptors. NIMH, Laboratory of Preclinical Pharmacology, Feb., 1982. 2 Is there an endogenous ligand for the 5HT2 receptor? American Society for Neuropsychopharmacology, San Juan, Puerto Rico, Dec., 1983. 3 Recent advances in the mechanism of antidepressants. National Naval Medical Center, Department of Psychiatry, Grand Rounds, April, 1984. 4 Evidence for an endacoid for the 5HT2 recognition site, NIMH, Laboratory of Preclinical Pharmacology, Washington, DC, April, 1984. 5 Evidence for distinct subcellular classes of opiate receptors. NIMH, Laboratory of Neurophysiology, 1985.

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6 The phosphoinositide-protein kinase C cascade. National Naval Medical Center, Department of Endocrinology,Grand Rounds, 1985. 7 Pharmacology support of the cardiovaculature in septic shock: experimental aspects. 8th Annual Shock Society Meeting, Baltimore, MD, June, 1985. 8 Alterations of receptor-effector coupling in septic shock. NIH, Department of Critical Care Medicine, 1985. 9 Vascular phosphoinositide metabolism hydrolysis and calcium channels. Armed Forces Radiobiological Research Institute, Division of Biochemistry, March 1986. 10 Receptor alterations in septic shock (or: Why catecholamines don't work!) National Naval Medical Center, Department of Critical Care Medicine, Grand Rounds, April 1986. 11 Septic shock: a disease of altered calcium metabolism.National Naval Medical Center, Department of Anesthesiology, August 1986. 12 Alterations in receptors and phosphoinositide metabolism in septic shock. Uniformed Services University School of the Health Sciences, Department of Neurobiology, Bethesda, MD, August 1986. 13 Phosphoinositide metabolism: clinical and experimental aspects. Smith, Kline and French Pharmaceutical Co. Department of Investigative Toxicology, Swedeland, PA October, 1986. 14 Biochemical mechanisms of serotonergic signal transduction. University of Michigan, Mental Health Research Institute,Department of Psychiatry, Ann Arbor, MI, January 1987. 15 Phosphoinositide metabolism: clinical and experimental aspects. Armed Forces Radiobiological Research Institute, Department of Physiology, April, 1987. 16 Regulation of smooth muscle contraction by phosphoinositide metabolism and protein kinase C. Berlex Pharmaceuticals, Inc., Department of Pharmacology, Cedar Knolls, NJ, September 1987. 17 5HT2 receptors and signal transduction. NIMH, Unit on Functional Neuroanatomy, Bethesda, MD, October 1987. 18 Alterations in hepatic and aortic adrenergic receptor mediated signal transduction in septic shock. NMRDC Conference on Molecular and Cellular Mechanisms of Septic Shock, Feb 29-March 1, 1988. 19 Molecular mechanisms of serotonergic signal transduction: role of protein kinase C. Department of Biochemistry, St. Louis University Medical Center, June 1988. 20 Molecular and Immunologic Approaches to Defining Serotonergic Signal Transduction. NIMH Unit of Functional Neuroanatomy, September 7, 1988. 21 5HT-receptor stimulated phosphoinositide metabolism and protein kinase C activaton, SEROTONIN: from cell biology to pharmacology (1st International Meeting of the Serotonin Club) Florence, Italy, March 1989. 22 Molecular and immunological approaches to studying serotonergic signal transduction. Department of Pharmacology, Texas Tech University School of Medicine, Lubbock, TX, February, 1989. 23 Alterations in 5HT receptors and receptor mRNA following antidepressant treatment. Psychiatric Research Society Meeting, Park City, Utah, March 1989. 24 Regulation of 5HT receptor gene expression. Satellite meeting of the ACNP, Maui, Hawaii, December 1989. 25 Regulation of 5HT receptor gene expression. Laboratory of Clinical Sciences, National Institute of Mental Health, Bethesda, MD, September, 1989. 26 Molecular mechanisms of serotonin receptor regulation. Department of Psychiatry, Case Western Reserve University Medical School, Cleveland, OH, February, 1990. 27 Developmental and synaptic regulation of serotonin receptors. 2nd International Serotonin

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Symposium, Basel, Switzerland, July 1990. 28 5-HT Receptors: from molecules to man. Grand Rounds in Psychiatry. Case Western Reserve University School of Medicine, October, 1991. 29 5-HT Receptors: an update. National Institute of Drug Abuse--Addiction Research Center, Baltimore, MD, February 20, 1992. 30 5-HT2 Receptors: molecular and biochemical studies. Department of Pharmacology. Case Western Reserve University Medical School, February 5, 1992. 31 5-HT2 Receptors: clinical and preclinical aspects. CINP Annual Meeting, Nice, France. July, 1992. 32 5-HT Receptors: Clinical and experimental aspects. CME Symposium sponsored by CPC Hospital, Tacoma, Washington, March 5, 1992. 33 Identification of receptor domains which modify ligand binding to serotonin receptors. Marrion-Merrill Dow Research Institute, Cincinnati, OH, July 13, 1992. 34 Serotonin receptor subtypes: basic and clinical aspects. VII Congress of the International Society of Greek Neuroscientists, Crete, September 6, 1992. 35 Identification of receptor domains which modify atypical antipsychotic drug binding. American College of Neuropsychopharmacology Annual Meeting, San Juan, December 11, 1992. 36 Serotonin receptors: an update. American Academy of Clinical Psychiatry Annual Meeting, Chicago, IL, October 7, 1993. 37 Serotonin receptors: molecular biology and signal transduction. Departments of Pharmacology and Medicinal Chemistry, October 22, 1993, Medical College of Virginia, Richmond, VA. 38 How do drugs bind to 5-HT receptors. Department of Biochemistry, Case Western Reserve University School of Medicine, October 15, 1993. 39 Serotonin receptor molecular biology. UpJohn Pharmaceutical Company, Kalamazoo, MI, March 25, 1994. 40 How do drugs bind to 5-HT receptors? Departments of Psychiatry and Neursciences, Vanderbilt University School of Medicine, Nashville, TN, July 22, 1994. 41 How drugs bind to 5-HT receptors: is it possible to design drugs by computer. Serotonin in Neurosciences, Global Business Enterprises, Philadelphia, PA, September 28, 1994. 42 What makes an atypical antipsychotic drug atypical? Serotonin in Neurosciences, Global Business Enterprises, Philadelphia, PA, September 29, 1994. 43 How drugs bind to 5-HT receptors. Annual Meeting of the American College of Neuropsychopharmacology, San Juan, Puerto Rico, December 13, 1994. 44 How drugs bind to 5-HT receptors and its relevance to schizophrenia. Western North Carolina Neuroscience Chapter, Bowman-Gray School of Medicine, Winston-Salem,NC. February 14,1995. 45. Basic and clinical aspects of multiple serotonin receptors. Grand Round in Psychiatry, Wayne State University School of Medicine, March 15, 1995. 46. How drugs bind to and regulate 5HT receptors. Serotonin in Neurosciences, Philadelphia, PA Jan. 1996. 47. How drugs bind to 5HT receptors. Department of Medicinal Chemistry, School of Pharmacy, University of Toledo, Toledo, OH. Feb 1, 1996. 48. Regulation of 5HT2A receptors: basic and clinical aspects. Department of Psychiatry, Stanford University School of Medicine, Stanford,CA Feb 29, 1996. 49. Interaction of atypical antipsychotic drugs with multiple neurotransmitter receptors. 8th International Catecholamine Meeting, Asilimor, CA, October, 1996.

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50. New insights into receptor regulation: 5HT2A receptors. ACNP Annual Meeting, San Juan, Puerto Rico, December, 1996. 51. New insights into structure-function aspects of 5HT2A receptors. Pharmacology, 1997 (ASPET), San Diego, CA, March 8, 1997. 52. Regulation of 5-HT2A and receptors and relevence for atypical antipsychotic drug actions. Department of Psychiatry, Yale University Medical School, May 12-13, 1997. 53. 10 Years of Serotonin Receptor Research: Molecular biology of serotonin receptors. Sponsored by the Society for Biological Psychiatry, Florida, Nov. 17-18, 1997. 54. Regulation of 5-HT2A receptors by agonists, antagonists and protein kinases. Department of Neurosciences, Vanderbilt University Medical School, Nov. 19, 1997. 55. Trafficking of 5-HT receptors. Satellite symposium on Receptor Trafficking at Society for Neurosciences Annual Meeting, New Orleans, LA. Oct. 25, 1997. 56. What makes an atypical antipsychotic drug atypical. Special Interest social on atypical antipsychotic drugs, Society for Neurosciences Annual Meeting, New Orleans, LA. Oct. 25, 1997. 57. Regulation of 5-HT2A receptors by antipsychotics and antidepressants. The New Neuropsychiatry Symposium, Cleveland, OH. Nov. 15, 1997. 58. Serotonin Receptors: Basic and Clinical Aspects. Department of Psychiatry Grand Rounds, University of South Florida Medical School, Jan 30, 1998. 59. Regulation of serotonin receptor trafficking by agonists, antagonists and protein kinases. NIDA Symposium, NIH, Feb 9, 1998. 60. Clozapine alters the subcellular distribution of 5-HT2A receptors. Annual Meeting of the

Society of Biological Psychiatry, Toronto, Canada, May, 1998. 61. Workshop on Psychopharmacology Directions. NIMH, Washington, DC, May 1998. 62. Endocytosis as a mode of 5-HT receptor regulation. IUPHAR Satellite Symposium on

serotonin. Rotterdam, July, 1998. 63. Structure-function studies of 5-HT2-family receptors. Merck Chemical Company, New

Jersey, Oct. 1998. 64. Are animal models needed in psychiatric research. Special Interest Social, Society for

Neurosciences Annual Meeting, Nov. 1998. 65. Structure and function of 5-HT2-family receptors. University of Massachusetts School of

Medicine, Jan 11, 1999. 66. Structure and function of 5-HT2A receptors. Loyola University School of Medicine,

Department of Neurosciences, Feb. 10, 1999. 67. Paradoxical regulation of 5-HT2A serotonin receptors. NIH/NIDA, Feb 22, 1999 68. Regulation of 5-HT2 receptor internalization. University of Michigan School of Medicine,

Departments of Psychiatry and Pharmacology, March 24, 1999. 69. Trafficking of 5-HT receptors. Great Lakes GPCR Retreat, London, Ontario, Canada, Nov 19, 1999 70. 5-HT2A receptors: paradoxes and opportunities. Roche Pharmaceuticals. Palo Alto, CA.

April,2000. 71. 5-HT2A receptors: paradoxes and opportunities. Department of Pharmacology,

Columbia University Medical School. April, 2000. 72. Receptors in motion: dancing atoms and molecules. Department of Pharmacology, Tufts

University Medical School June 1, 2000. 73. Structure-function of G-protein coupled receptors. ASPET Mini-Course on Receptors.

ASPET/ASBMB Annual Meeting, June 3, 2000 . 74. 5-HT2A receptor internalization. Neuropet 2000, Columbia University, June 2000. 75. The role of 5-HT2A and 5-HT2C receptors in atypical antipsychotic drug actions. CINP,

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Brussels, Belgium, July, 2000. 76. 5-HT2A receptor internalization: paradoxes and opportunities. St. Louis University

Medical School Department of Biochemistry, St. Louis, MO, Sept. 2000. 77. 5HT2A receptors: paradoxes and opportunities. Society for Neurosciences Annual

Meeting Symposium on 5HT receptors. Nov 2000 . 78. Targeting and trafficking of 5-HT receptors. Serotonin Club Meeting, New Orleans, LA,

Nov 2000. 79. 5-HT receptors in motion. UNC-Chapel Hill, Department of Neurosciences, 22 Feb

2001. 80. 5-HT receptors in motion. Medical College of Virginia, Department of Medicinal

Chemistry, May 1, 2001. 81. How do atypical antipsychotic drugs really work? Ohio Psychiatric Association Meeting,

Oct 20, 2001. 82. 5HT receptors in motion. Synaptic Pharmaceutical, Inc. Oct 31, 2001. 83. 5HT receptors in motion. Department of Psychiatry, University of Iowa School of

Medicine, Dec 2, 2001. 84. What makes an atypical antipsychotic drug atypical? Grand Rounds in Psychiatry,

Department of Psychiatry, University of Iowa School of Medicine, Dec 3, 2001. 85. Aripiprazole: a serotonin-dopamine system stabilizer. VISION World-wide Bipolar

Summit. Puerto Rico, March 7, 2002. 86. 5HT receptors in motion. Department of Pharmacology, Northwestern University Medical

School, March 8, 2002. 87. Pharmacology for a new millennium. International PET Symposium. Turku, Finland. May

27, 2002. 88. 5-HT receptors in motion. Cleveland Clinic Foundation Program in Cell Biology Seminar

Series, May 3, 2002 89. 5-HT receptors in motion. Department of Pharmacology, University of Washington

School of Medicine, May 7, 2002 90. What makes an atypical antipsychotic drug atypical? Department of Psychiatry—

Harborview Medical Center (University of Washington), Seattle, Washington, May 8, 2002.

91. Dopamine-Serotonin System Stabilization: What Is It and What Does It Mean? Treatment of Psychotic Disorders: What is the State of the Art? New York, July 12, 2002.

92. Paradoxical targeting and trafficking of 5-HT2A serotonin receptors. Arena Pharmaceuticals, August 16, 2002.

93. NMDA antagonists in the treatment of bipolar disorder. Forest Pharmaceuticals Scientific Advisory Board Meeting, Sept 26,2002.

94. Preclinical pharmacology of aripiprazole. APA-IPS Meeting, Chicago, Il; Oct 11, 2002. 95. Screening the receptosome uncovers novel targets for drug discovery. Great Lakes

GPCR Meeting, Ann Arbor,MI, October 19, 2002. 96. Screening the receptosome uncovers novel targets for drug discovery. Center for Drug

Discovery, Georgetown University Medical School; October 23,2002. 97. Preclinical pharmacology of isotretinoin and derivatives. NIMH Workshopon Retinoids

During Development, Washington DC, November 19, 2002. 98. Screening the receptosome uncovers novel targets for drug discovery. Departments of

Psychiatry and Pharmacology, University of North Carolina School of Medicine, Chapel Hill, NC, Nov 26, 2002

99. Preclinical pharmacology of aripiprazole. Eli Lilly workshop, San Juan, PR, Dec 8, 2002.

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100. Issues in occupancy for PET ligands, Workshop at American College of Neuropsychopharmacology Annual Meeting, December 11, 2002.

101. Plasticity of 5-HT2A receptors. Panel talk at American College of Neuropsychopharmacology Annual Meeting, December 12, 2002.

102. 5-HT2A receptor signal transduction. American Society for Pharmacology and Experimental Therapeutics Annual Meeting (FASEB), San Diego, CA April 12, 2003.

103. Screening the receptorome reveals unexpected targets of psychoactive drug actions. Center for Basic Neurosciences and Department of Psychiatry, Unversity of Texas Southwestern Medical School, April 22, 2003.

104. Novel mechanisms of action of atypical antipsychotic drugs. American Psychiatric Society Annual Meeting, San Francisco, May 20, 2003.

105. Screening the receptorome reveals unexpected targets for drug discovery. New Clinical Drug Evaluation Unit (NCDEU) Annual Meeting, Boca Raton May 27, 2003.

106. Targeting and trafficking of 5-HT2A serotonin receptors. University of Illinois-Chicago,

May 28, 2003. 107. Screening the receptorome reveals validate targets for drug discovery.

Psychogenomics, Inc. (New Jersey); June 17,2003. 108. Serotonin receptors as targets for cognitive enhancing medications. MATRICS meeting

(NIH/FDA conference); June 23, 2003. 109. Screening the receptorome reveals unexpected targets for antipsychotic drug actions.

Grand Rounds Columbia University Psychiatry Department. June 27, 2003. 110. Screening the receptorome reveals unexpected targets for antipsychotic drug actions.

Duke University CNS Summit, Boca Raton, FL, July 27, 2003. 111. The NIMH Psychoactive Drug Screening Program. Molecular Libraries Meeting

(NIMH/NIDA/NINDS)—special director’s fund initiative planning meeting. Aug 11, 2003. 112. Screening the receptorome to discover molecular targets responsible for psychoactive

drug actions. Psychoactive Botanical Products Workshop, sponsored by NIDA and the Office of Dietary Supplements, NIH. Sept 9, 2003.

113. Screening the receptorome to discover validated targets for anorectic drug discovery. Bristol-Myers Squibb, Princeton NJ Sept 25, 2003.

114. Screening the receptorome reveals unexpected molecular targets for psychostimulant drug actions. NIDA Workshop: Serotonin and Dopamine: Interactive Contributions to Psychostimulant Reward and Aversion. Rockville, MD Sept 29, 2003.

115. Screening the receptorome reveals novel targets for CNS drug discovery. Northeast Ohio University College of Medicine Pharmacology Series Seminar, Oct 13, 2003.

116. Molecular mechanisms responsible for antipsychotic-drug induced diabetes. American Diabetes Association Consensus conference, Arlington, VA Nov 18, 2003.

117. Mechanism of action of partial agonists in schizophrenia. National Network of Psychiatric Educators, Orlando, FL Nov 21, 2003.

118. Molecular mechanisms responsible for anorectic-drug induced valvular heart disease. Cardiovascular Safety Advisory Board Meeting, Pfizer Pharmaceuticals, Boston, MA. December 16, 2003.

119. Screening the receptorome to discover validated targets for cognition-enhancing small molecules. Memory Pharmaceuticals, Inc. Jan 20, 2004.

120. 5-HT2A receptor targeting and trafficking: what a long, strange trip its been. Department of Pharmacology, University of Melbourne Medical School, Jan 27, 2004.

121. Screening the receptorome to discover validated molecular targets for CNS drug discovery. Australian Society of Neurosciences Annual Meeting, Symposium on

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GPCRs, Jan 29, 2004. 122. New options in the treatment of bipolar mania. Distance Learning Network, Feb 24, 2004 123. Screening the receptorome to discover validated molecular targets for drug discovery.

Louisiana State University Medical School, Department of Pharmacology, March 16, 2004.

124. NIMH Psychoactive Drug Screening Program and Molecular Libraries Initiative. Academy of Molecular Imaging Annual Meeting, March 27, 2004.

125. Targeting and trafficking of 5-HT2A serotonin receptors: what a long, strange trip its been. Departments of Neurosciences and Pharmacology, University of Georgia, Athens, April 29, 2004.

126. Screening the receptorome to discover molecular targets responsible for drug toxicities. NIH Summit on Predictive Toxicology, Bethedsa, June 15, 2004.

127. Drug selectivity: in vitro and in silico methods. Annual Meeting of the Society of Nuclear Medicine; Workshop in receptor binding kinetics. June 20, 2004

128. 5-HT2-family receptors: from atoms to patients. CINP Symposium on 5-HT2 receptors.

Paris, June 22, 2004. 129. Grand rounds in Psychiatry: From preclinical studies to antipsychotic drug actions.

Oklahoma University School of the Health Sciences, Oklahoma City, OK, Sept 9, 2004. 130. Mining the receptorome: in silico and physical screening of the receptorome yields novel

insights into CNS drug discovery and target validation BRAIN MAPS AND SYSTEMS BIOLOGY: INTEGRATION WITH THE MAN BRAIN PROJECT, Satellite meeting of the Society for Neurosciences Meeting, San Diego, CA Nov 22, 2004.

131. 5-HT receptor targeting and trafficking: what a long, strange trip its been. Department of Pharmacology, LSU Medical School, Dec 7, 2004.

132. Why non-selective drugs are superior to selective ones for mood disorders. American College of Neuropsychopharmacology Annual Meeting, San Juan Puerto Rico, Dec 15, 2004

133. Mining the receptorome. American College of Neuropsychopharmacology Annual Meeting, San Juan Puerto Rico, Dec 15, 2004.

134. Magic shotguns vs magic bullets. Advances in Translational Research for CNS Diseases. Orlando, FL Jan 24, 2005

135. Mining the receptorome. Yale University BSTP Distinguished Lecture Series, Department of Psychiatry, New Haven, CT March 21, 2005

136. The comparison of atypical antipsychotic’s action for the ideal treatment. 2005 Annual Spring Meeting of the Korean College of Neuropsychopharmacology, Korea, March 24, 2005

137. Serotonin receptor interacting proteins (in symposium devoted to 5-HT and DA interacting proteins) International Congress of Schizophrenia Meeting, Savanna, GA April 4, 2005

138. Is functional selectivity an in vitro artifact? (in symposium on Functional Selectivity) ASPET/FASEB Annual Meeting, San Diego, April 5, 2005

139. Mining the receptorome for drug discovery (in symposium on Novel Screening Approaches for Drug Discovery), ASPET/FASEB Annual Meeting, San Diego CA, April 6, 2005.

140. Mining the receptorome Reveals Validated Molecular Targets for CNS Drug Discovery. Keynote Speaker, 3rd Annual Psychiatric Drug Discovery and Development Meeting, Princeton, NJ, April 12, 2005.

141. Mining the receptorome for CNS Drug Discovery, Chancy Leake Memorial Lecture,

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University of Texas Medical Branch, Department of Pharmacology, Galveston, TX, April 15, 2005.

142. 5-HT2A receptor targeting: what a long, strange trip it’s been. Department of Pharmacology, University of Tennessee Health Sciences Center, Memphis, TN April 27, 2005.

143. Mining the receptorome. Pharmaceutical Sciences and Pharmacogenomics Graduate Program. UCSF, May 11, 2005.

144. Mining the receptorome for CNS Drug Discovery. Department of Psychiatry, Harvard University Medical School, McLean Hospital, June 21, 2005

145. Mining the receptorome for CNS Drug Discovery. Envivo Pharmaceuticals, Boston MA, June 22, 2005

146. Mining the receptorome: an effective approach for discovering structurally novel leads. Center for Molecular Libraries Development Annual Symposium. Boston, MA June 24, 2005.

147. Molecular mechanisms for salvinorin A binding KORs. International Narcotics Research

Conference Symposium on New Opioid Compounds. Annapolis, MD July 14, 2005. 148. 5-HT2A receptors and PML: functional considerations. International Viral Meeting,

Providence, RI Sept 14, 2005. 149. Mining the receptorome: a highly efficient method for molecular target discovery and

validation. Mayo Clinic Jacksonville, Division of Neurosciences, Sept 16, 2005. 150. Mining the receptorome: a highly efficient method for molecular target discovery and

validation. 8th International IMCPP Meeting, Oxford University, Oxford, UK. Sept 26, 2005.

151. Identification of molecular targets responsible for antipsychotic-drug induced weight gain. NIMH Conference on Metabolic Consequences of Antipsychotic and Mood Stabilizing Agents, Washington University, October 11,2005.

152. Functional selectivity: opportunity or obfuscation. Abbott Labs, CNS Discovery Group, Abbott Park, Ill October 17, 2005.

153. Mining the receptorome: an efficient approach for molecular target discovery. University of North Carolina, Chapel Hill, Department of Pharmacology. October 19, 2005.

154. Mining the receptorome: an efficient approach for molecular target discovery. 6th Great Lakes GPCR Conference, Montreal, CA October 22, 2005.

155. Mining the receptorome to discover and validate molecular targets for CNS drug discovery. Frontiers in Psychiatry Lecture, AstraZenica, Wilmington DE, Nov 4, 2005.

156. Caveolin-1 profoundly modulates GPCR signaling. Symposium on Lipid Rafts, Society for Neurosciences Annual Meeting, Washington, DC, Nov 14, 2005.

157. Caveolin profoundly modulates GPCR signaling. Symposium on Lipid Rafts, ACNP Annual Meeting, Hawaii, Dec 14, 2005.

158. Mining the receptorome: an efficient approach for CNS drug discovery. School of Pharmacy, Florida A&M University, March 23, 2006.

159. Caveolin and RSK2: the yin and yang of 5-HT2A signaling. Ray Fuller Symposium, FASEB Meeting, San Francisco, CA April 2, 2006.

160. Building RASSL’s with directed evolution. Engineering RASSLS Meeting, Gladstone Institute, UCSF, April 6, 2006.

161. Mining the receptorome for CNS drug discovery. Drexel University Department of Pharmacology, April 24, 2006.

162. Selectively non-selective drugs for schizophrenia. CINP Annual Meeting, 2006 163. RSK2 exerts a tonic brake on 5-HT receptor signaling. 5-HT Club International Meeting,

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Sapporo Japan, July 2006. 164. Magic shotguns vs Magic bullets for CNS drug Discovery. American Chemical Society

Annual Meeting, San Francisco CA Sept 11, 2006. 165. Repositioning in the public sector. Drug Repositioning Summit, Boston Oct 17, 2006 166. Small molecule approaches for obesity drug discovery. GlaxoSmithKline, RTP, Oct 25,

2006. 167. Salvinorin A: history and molecular Pharmacology. ACNP Annual Meeting, Panel

Presentation on Salvinorin A and k-opioid receptors. Hollywood, FL Dec 2006 168. Antipsychotic drug discovery: peril or potential. ACNP Annual Meeting Panel on Drug

Discovery, Hollywood FL Dec 2006. 169. Selective drugs or evolved receptors:how best to modulate neuronal activity. Department

of Pharmacology, Vanderbilt University, Dec 13, 2006. 170. Selective drugs or evolved receptors: how best to modulate CNS activity. Gordon

Research Conference on Molecular Pharmacology. Ventura, California, Jan 30, 2007. 171. Selective drugs or evolved receptors: how best to modulate CNS activity. Medical

College of Georgia, Department of Pharmacology, Feb 8, 2007. 172. Selective drugs or evolved receptors? Kansas University Drug Discovery Symposium,

March 13, 2007. 173. 5-HT2A receptors and JC Virus. Biogen, April 6, 2007, Boston, MA. 174. Selective drugs or evolved receptors? ACS Perspectives, Boston, MA April 30, 2007. 175. Mining the receptorome: a powerful approach for target discovery and validation. AMRI,

May 3, 2007. 176. Massively parallel screening of the receptorome. Gordon Research Conference on G

proteins and Protein Phosphorylation. June 10, 2007. 177. Selectively non-selective drugs or evolved receptors? Joint symposium by American

Chemical Society, UCSD and Johnson&Johnson, June 19, 2007. 178. Receptorome screening for repurposing. ACS Symposium on Repurposing, Boston, MA

August 2007. 179. Selective drugs or evolved receptors. Cornell University Department of Pharmacology,

NY, NY Sept 4, 2007. 180. Plenary Lecture Roche Global Medicinal Chemistry Meeting, Roche Palo Alto, Sept 17,

2007. 181. Mining the receptorome: a powerful approach for target discovery and validation.

Prestige Lecture, Universite de Montreal, Montreal, Canada. Oct 11, 2007. 182. Featured Lecture. Mining the receptorome: a powerful approach for target discovery and

validation. Assays and Cellular Targets Meeting. San Diego, CA Oct 16, 2007. 183. Mining the Recepterome: An Efficient Approach for Target Discovery and Validation.

Anti-Cancer Drug Discovery and Development Retreat held at the University of Pennsylvania on December 7 in Philadelphia.

184. Modulating neuronal signaling with evolved GPCRs. ACNP Annual Meeting, December 2007.

185. Selective drugs or evolved receptors: how best to modulate neuronal signaling. Scripps Neuroscience Seminar Series, Jan 30,2008

186. Selective drugs or evolved receptors: how best to modulate signaling in vivo. Department of Pharmacology, University of Oslo, Norway, Feb 29, 2008.

187. Mining the receptorome: a powerful chemical biology approach for target discovery and validation. Department of Pharmacology and Chemical Biology. Mount Sinai Medical School, March 28, 2008.

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188. Chemical and synthetic biological approaches to regulating signal transduction. Department of Pharmacology, Georgetown University, May 6, 2008.

189. Phenotypic and parallel approaches to cancer cell drug discovery. 32nd Lineberger Cancer Center Symposium, May 13, 2008.

190. Phenotypic and massively parallel approaches to drug discovery. Chapel Hill Drug Discovery Meeting. May 16, 2008.

191. Synthetic biologic approaches for spatio-temporal regulation of signal transduction. 21st Annual Chicago Signal Transduction Symposium. May 22, 2008.

192. Drugs, valvular heart disease and the treatment of prolactin tumors. ENDO 2008 (Endocrine Society Annual Meeting), June 15, 2008.

193. Molecular targets for enhancing cognition in schizophrenia. CINP 2008 Symposium, Munich, July 15, 2008.

194. Atypical antipsychotic drug pharmacology: what is the state of the art and where are we going? CINP 2008 Symposium, Munich, July 16, 2008.

195. Modulation of 5-HT2 signal transduction by protein kinases and scaffolding proteins in vivo. Serotonin Club International Meeing, 2008. Oxford, UK, July 20, 2008.

196. Serotonergic drugs and valvular heart disease. International Clinical Pharmacology and Therapeutics, Quebec City, Quebec. July 29, 2008

197. Mechanisms of GPCR functional selectivity. Invitrogen GPCR Conference on Allosterism and GPCR functional selectivity. Madison, WI Sept 10, 2008.

198. Mining the receptorome: an efficient approach for molecular target identification and validation. Hamner Institute, RTI, NC Sept 19, 2008.

199. Drugs and valvular heart disease. US FDA, Sept 29, 2008 200. Using evolved receptors to modulate neuronal signaling. Genetic Manipulation of

Neuronal Activity, Janelia Farms (HHMI), Nov 4, 2008. 201. Do 5-HT2A and mGluR2 provide interacting or independent targets for antipsychotic

drug discovery. ACNP Panel on Novel Mechanisms for Antipsychotic Drug Discovery, Dec 9, 2008.

202. Molecular, Cellular and Behavioral Determinants for Functional Selectivity for serotonin and opioid receptors. ACNP Panel on Functional Selectivity of GPCRs. Dec 11, 2008.

203. Remote control of neuronal signaling. National Institute of Drug Abuse—IRC Baltimore, MD. March 3, 2009.

204. Chemical and synthetic biological approaches to controlling neuronal signaling. UCSF Chemical Biology Program. March 12, 2009.

205. DREADDs to control neuronal signaling. DREADD/RASSL user group meeting. UCSF, March 13, 2009.

206. Plenary Lecuture, Frontiers in Neurosciences, Medical University of South Carolina, Department of Neurosciences, March 20, 2009.

207. Mining the receptorome. RTI, March 24, 2009. 208. Mining the receptorome. ASBMB Annual Meeting Symposium on Drug Discovery and

Chemical Biology (Brian Schoichet Chair). April 22, 2009. 209. Mining the receptorome. Grand Rounds in Psychiatry, University of Pittsburgh Medical

School. May 8, 2009. 210. Mining the peptide-receporome. NIDA Peptidome meeting. May 21, 2009. 211. Remote control of neuronal signaling. Gordon Research Conference on Molecular

Pharmacology, Italy, May 29, 2009. 212. Remote control of neuronal signaling. NIDA Chemical Genomics Meeting, Portland

Oregon, July 17, 2009.

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213. NIMH Chemical Biology Satellite Symposium, SFN Annual Meeting, 16 October 2009 214. Mining the receptorome. GPCR Great Lakes Symposium, Rochester, NY 17 October

2009 215. New approaches for GPCR and ion channel screening. IDREAM Conference, San Diego

18 November 2009. 216. Role of caveolin in atypical antipsychotic drug actions. ACNP Annual Meeting Panel

Presentation 7 December 2009. 217. Pharmacology of atypical antipsychotic drugs. ACNP Annual Meeting Study Group 8

December 2009. 218. Remote control of Neuronal activity. Harvard Endocrinology Department, January 22,

2010. 219. Atypical antipsychotic drug actions. Lowenthal Lecture, Medical College of Virginia

Neurosciences and School of Pharmacy Neurosciences Retreat. 19 March 2010. 220. Remote control of neuronal signaling.UCSF Gallo Research Center. 31 March 2010. 221. Remote control of neuronal singaling and antipsychotic drug discovery. Broad (Harvard-

MIT) Institute, Stanly Center, 21 April 2010. 222. Novel approaches to CNS drug discovery. Axelrod Symposium ASPET Annual meeting,

San Diego 26 April 2010. 223. Using evolved GPCRs to remotely control cellular signaling, IEEE Meeting Symposium

on Membrane Proteins, Thomas Jefferson University, June 2, 2010. 224. Functional selectivity: a novel approach for CNS drug discovery. CICBDD Drug

Discovery Meeting, Chapel Hill, June 9, 2010. 225. Plenary Lecture ‘Neurobiology of Schizophrenia’, Merck CNS Global Expert Forum,

Philadelphia, PA June 29, 2010. 226. Irving Page Lecture, Serotonin Club Meeting Montreal, CA 1 July 2010 227. Novel approaches for Drug Discovery. 21st Century Bioscience Meeting, University of

Buffalo, Sept 11, 2010 228. New approaches for GPCR Drug Discovery. SBS Regional Meeting, RTP, North

Carolina, October 16, 2010 229. Chemical Genetic Approach for remotely controlling neuronal signaling. HHMI Janelia

Conference, Nov 9, 2010 230. Chemical Genetic Approach for remotely controlling neuronal signaling, Department of

Medicinal Chemistry, Medical University of South Carolina, Nov 30, 2010 231. Discovering novel targets for approved drugs. ACNP Panel on CNS Drug Discovery,

Dec 7, 2010 232. Chemical Genetic Approach for remotely controlling neuronal signaling, Department of

Neuroscience, UCSD, Feb 9, 2011 233. New approaches for CNS drug discovery, University of Utah Brain Symposium, March

11, 2011 234. Novel approaches for CNS drug discovery; Keystone Conference on Early Stage Drug

Discovery; Snowbird Utah April 5, 2011 235. Molecular repurposing; ASPET Symposium on Drug Discovery; April 11, 2011 236. Chemical genetic approach for remotely controlling neuronal signaling, Department of

Psychiatry, University of Texas Southwestern Medical School April 27, 2011 237. Chemical genetic approach for remotely controlling neuronal signaling, Department of

Neuroscience, University of Maryland Medical School May 5, 2011. 238. NIH Repurposing Meeting; Office of the Director NIH April 21-22, 2011 239. Chemical genetic approach for remotely controlling neuronal signaling, Department of

Neuroscience, University of Oregon, Eugene 19 May 2011

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240. Chemical genetic approach for remotely controlling neuronal signaling, Department of Pharmacology, LSU Medical School, 26 May 2011

241. Molecular repurposing, Gordon Conference on HTS, June 2011 242. Molecular repurposing, IECB Meeting France, 2011 243. Chemical genetic approach for remotely controlling neuronal signaling, NIEHS, NIH,

Sept 2011 244. Chemical genetic approach for remotely controlling neuronal signaling, Duke

Neurobiology, Sept 2011 245. New approaches to drug discovery. Amgen, Oct 2011. 246. New Molecules for New Targets: Identifying Novel Ligands for Cannabinoid Receptors

and TRP Channels. CCC 2011, RTP 29 October 2011. 247. Novel approaches to treat psychosis in Parkinson’s Disease. Parkinson’s Disease

Association Foundation Meeting, Washington DC, 11 Nov 2011. 248. Parallel profiling of orphan GPCRs on a genome-wide scale. Conformetrix GPCR

Workshop, Maui, Hawaii, Dec 6, 2011. 249. Columbia University Psychiatry Grand Rounds and Workshop on DREADDs. March 9,

2012 250. Chemical and Synthetic Biology meets GPCRs: Translational Implications. Protein

Phosphorylation and G Protein Gordon Conference, June 14, 2012 251. Chemical and synthetic biology approach for GPCR Structure. NIH Conference on

opioid receptor structure. NIH July 13, 2012 252. Chemical and synthetic biology meets opioid receptors. Keynote Speaker, INRC Annual

Meeting, July 18, 2012. 253. New approaches for drug discovery. Xth International Catecholamine Conference,

Asilomar California September 6, 2012. 254. Why academic drug discovery makes sense. University of Virginia Keynote Speaker for

drug discovery forum. Sept. 20, 2012 255. New technologies and tools. Plenary Speaker, Brain Research Optogenetics and

Pharmacogenetics Conference, Oct 11, 2012. 256. New approaches to psychiatric drug discovery. 20th Plenary Speaker, World Congress of

Psychiatric Genetics, Plenary Speaker, Hamburg Germany, 16 Oct 2012 257. Chemical and synthetic biology meet neural circuitry. Distinguished Lecturer –University

of Toronto Neurosciences. Nov 1, 2012 258. Chemical and synthetic biology meet neural circuitry. Department of Pharmacology,

University of Pennsylvania Dec 3, 2012. 259. Serotonin receptors, drugs and valvular heart disease: molecular aspects.

Cardiovascular Research Center Symposium. Duke University. Jan 12, 2013. 260. Chemical and synthetic biology meet neural circuitry. Johns Hopkins Neuroscience

Department, Jan 31, 2013 261. Chemical and synthetic biology meet neural circuitry. Thomas Jefferson Neuroscience, 5

Feb 2013. 262. Chemical and synthetic biology meet neural circuitry, Department of Pharmacology,

West Virginia University Medical School, 11 April 2013. 263. Chemical and synthetic biology meet neural circuitry Department of Neurosciences, Mt

Sinai School of Medicine, NYC 23 May 2013. 264. Chemical and synthetic biology meet neural circuitry, Causal Neuroscience FENS

Course, Bertinoro Italy, 30 May 2013. 265. 23rd Solvay Chemistry Conference 17 October 2013 266. Chemical and synthetic biology meet neural circuitry, Dystonia Foundation, NYC 28

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October 2013. 267. DREADD technology, Society of Neurosciences Short Course on chemo- and

optogenetics 8 Nov 2013 268. Transforming translational neurosciences, Meet the Expert, SFN 9 Nov 2013 269. SFN Special lecture: “How synthetic and chemical biology will transform neuroscience”

SFN Annual meeting 11 Nov 2013. 270. How chemical and synthetic biology can transform neuroscience. University of Utah

Medical School. 14 Jan 2014 271. How chemical biology and chemogenetics can transform translational medicine.

Novartis, Cambridge, MA 29 Jan 2014 272. How chemical biology and chemogenetics can transform translational medicine.

University Hospitals of Cleveland Annual Neurosciences Research Keynote Lecture 15 April 2014

273. Chemogenetics: a transformational technology for neuroscience, Labroots Neuroscience Program 19 March 2014 (http://labroots.com/user/webinars/details/id/205 )

274. How chemical biology and chemogenetics can transform neuroscience. Swammerdam Lecture, Amsterdam, Netherlands, 26 May 2014

275. Novel psychoactive substances - understanding the pharmacological basis of their clinical effects and toxicity. Plenary Lecture European Association of Poisons Centres and Clinical Toxicologists Meeting 28 May 2014.

276. Chemical biology and safety pharmacology. US FDA 10 June 2014 277. Chemical biology and Chemogenetics. Center for Mental Health Research and Recovery

Meeting. Big Sky, MT 27 July 2014 278. Chemical and synthetic biology approaches for novel autism therapeutics. Simon

Foundation Meeting on Autism Therapeutics. 2 Sept 2014 279. How chemical and synthetic biology are transforming science. UNC Wilmington

Department of Chemistry 19 Sept 2014 280. Structural features responsible for functional selectivity. NYAS Symposium on GPCR

Functional Selectivity 30 Sept 2014 281. Transforming GPCR-ology. Hyman Nyznik Memorial Lecture. Great Lakes GPCR

Meeting 2 Oct 2014 282. How chemical and synthetic biology are transforming translational medicine. Merck

Pharmaceuticals, 7 Oct 2014. 283. How chemical and synthetic biology are transforming translational medicine.

Cardiovascular Research Group, Massachusetts General Hospital, Harvard Medical School, 14 Oct 2014.

284. How chemical and synthetic biology are transforming translational neuroscience. Department of Psychiatry Grand Rounds, Northwestern University Medical School, 22 Oct 2014.

285. How chemical and synthetic biology are transforming translational neuroscience. Plenary Lecture, Society of Molecular Psychiatry meeting, San Francisco, 7 Nov 2014.

286. Genome-wide approaches to GPCR drug discovery. Philip S Portoghese Lecture, University of Minnesota School of Pharmacy, 10 March 2015.

287. Update of DREADD technology. LABROOTS Neuroscience Webinar. 18 March 2015. 288. DREADD2.0: an enhanced chemogenetic technology. Experimental Biology Symposium

on new approaches for neuroscience research. Chicago, 30 March 2015 289. Structural features for functional selectivity. Experimental Biology Symposium on Biased

Signaling. Chicago, 31 March 2015 290. Interrogating the subterranean GPCR-ome. Department of Chemistry, Stanford

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University, 6 April 2015. 291. New technologies for illuminating brain actions. Department of Neuroscience, Baylor

University Medical School, 15 May 2015. 292. Illuminating the subterranean GPCR-ome. Pfizer Gene Family Forum, Rye NY 2 June

2015 293. Discovering allosteric modulators for the dark matter of the GPCR-ome. Bioorganic

Chemistry Gordon Conference 11 June 2015 294. Illuminating a subterranean GPCR-ome. Roche Brain Talks, Basel Switzerland, Sept 8

2015. 295. Illuminating a subterranean GPCR-ome. Department of Biochemistry, Duke University

Medical School, 18 Sept 2015. 296. Illuminating a subterranean GPCR-ome. Discovery on-target Keynote Address, Boston,

22 Sept 2015 297. Illuminating a subterranenean chemical(neuro)biology. Neuroscience Program. UNC

Chapel Hill, 24 September 2015. 298. Chemogenetics: a robust translational tool. American Neurological Society Annual

Meeting Symposium on Circuits, 26 September 2015. 299. Illuminating a subterreanean GPCR-ome. UCSF Chemical Biology, School of

Pharmaceutical Sciences, Oct 13, 2015 300. Illuminating a subterranean GPCR-ome; CHPS 2015 Drug Discovery Symposium, Oct

15, 2015 301. Chemogenetics, National Academy of Medicine Interest Group Meeting, 18 October

2015 302. Illuminating a subterranean druggable genome. Innovations in Biological Computing.

Chapel Hill 27 October 2015 303. Illuminating a subterranean GPCR-ome. Goodman Lecture, OHSU, Portland, Oregon 5

November 2015. 304. New tools for neuroscience. Neurotech 2015, MIT Nov 17, 2015 305. Chemogenetic and synthetic biology approaches for neurotherapeutics. Duke

Neurogenetics Symposium, Nov 23, 2015. 306. Illuminating a subterranean GPCR-ome, 90th Anniversary Symposium Physiology

Department, Vanderbilt University, 3 December 2015. 307. Illuminating a subterranean pharmacology. Koppyani Lecture, Georgetown University

Department of Pharmacology, 17 December 2015. 308. Illuminating a subterranean pharmacology, Keystone GPCR meeting, Feb 2016 (invited

talk but given by postdoc at last minute due to conflict) 309. Illuminating the hidden GPCR-ome. ASPET Symposium on GPCRs, San Diego April 3,

2016 310. Goodman and Gilman Award Lecture, ASPET, San Deigo April 3, 2016. 311. How atomic level understanding of GPCR structure transforms therapeutics. Universtiy

of Texas, Austin, April 14, 2016. 312. Strongwater Endowed Lecture, Rutgers Behavioral Research, April 21, 2016. 313. Keynote Lecture, Universtiy of Texas San Antonio Medical School Center for Biomedical

Neuroscience Program, May 6, 2016. 314. New insights into opioid receptor structure and function. Chemistry and pharmacology of

drug abuse meeting. Boston, MA June 2, 2016. 315. Keynote talk G protein workshop, Rockefeller University, June 14, 2016 316. Chemogenetics update. FASEB Summer Research meeting; Saxton VT. June 22, 2016. 317. Webinar on multiplexing technologies; BRAIN Technology development; July 25, 2016.

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318. Structure-Guided Discovery of Novel GPCR Therapeutics, Yale Neurosciences September 19, 2016

319. Structure-guided and structure-inspired discovery of novel GPCR therapeutics. Harvard Biochemistry and Pharmacology, September 29, 2016.

320. Towards a molecular understanding of drug action at GPCRs. Keynote address, Case Western Reserve University Department of Pharmacology retreat. October 6, 2016

321. Creating GPCR therapeutics from atomic level insights. Great Lakes GPCR Conference, Chicago, Oct 14, 2016.

322. Illuminating the hidden GPCR-ome. New York Academy of Sciences Chemical Biology Meeting. October 25, 2016.

323. Molecular mechanisms of drug actions. 4th Pritchard Memorial Lecture, University of Maryland Medical School, November 1, 2016

324. Chemogenetics as a circuitry-based tool kit. NIMH Advisory Board Meeting, Feb 9, 2017 325. Illuminating the druggable GPCR-ome. Pharmacogenomics Consortium Meeting.

London, March 2, 2017 326. Molecular insights into psychoactive drug action. Molecular Pharmacology Gordon

Research Conference. March 14, 2017. 327. New approaches for GPCR research. ASPET Presidential Symposium, 22 April 2017 328. Sigma-Aldrich Lectures, St.Louis, 4 May 2017 329. Martin Rodbell Lecture, NIEHS/NIH 16 May 2017 330. Towards a molecular understanding of psychoactive drug actions. Keynote

speaker,University of Pittsburgh Medical School Department of Pharmacology, 2 June 2017.

331. New insights into allosteric modulation of GPCRs. Gordon Research Conference on Proteins, 21 June 2017

332. Illuminating the druggable GPCR-ome. Department of Pharmacology, University of Pennsylvania Medical School 12 July 2017

333. New chemogenetic tools and technologies. NIMH Circuitry Meeting, Rockville MD 11 September 2017

334. Illuminating the druggable GPCR-ome. First Elliott Vessel Talk. Penn State University Medical School 27 September 2017

335. Illuminating the druggable GPCR-ome. Keynote Presentation ASPET/ADDC Colloquium. NIH Satcher Auditorim 19 October 2017

336. New tools and technologies for serotonin receptors. Great Lakes GPCR meeting. Ottawa, Canada 20 October 2017

337. Illuminating the druggable GPCR-ome. NYAS Chemical Neurobiology meeting. New York, 17 November 2017.

338. Illuminating the druggable GPCR-ome. 2018 Keystone meeting on GPCRs. New Mexicoo Feb 2018

339. Illuminating the druggable GPCR-ome. University of New Mexico Medical School, 15 Feb 2018

340. How insights into GPCR structure accelerate drug discovery. VCU Medicinal Chemistry, 7 March 2018

341. How insights into GPCR structure accerate drug discovery. Temple University Medical School, April 3, 2018.

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CURRENT GRANTS/CONTRACTS (Approximate amounts listed) 2017-2023: U24DK116195: Scalable technologies for illuminating the druggable GPCR-ome. UNC Chapel Hill. BL Roth and BK Shoichet (MPI) $13,600,000 (approximate) 2016-2021: RO1MH112205: Molecular details of psychoactive drug actions. UNC Chapel Hill. BL Roth and BK Shoichet (MPI) $3,200,000 (approximate) 2014-2019: PO1DA035764-01A1 Structure-function of opioid receptors, Scripps and UNC RC Stevens and BL Roth Co-PI’s $7,500,000 (approximate total award) 2013-2018 HSSN-71-2008-0005C NIMH Psychoactive Drug Screening Program Continuation of NO1MH32004, UNC Chapel Hill Medical School BL Roth,PI 30% Effort $12,000,000 (Approximate depending on milestones; Awarded Sept 2013) 2018-2023 RO1DA045657: Mechanistic insights into LSD actions at 5-HT2A serotonin receptors. BL Roth PI 15% effort $3,225,000 (approximate total) PRIOR GRANTS RECEIVED 1984-88 Independent investigator at the Naval Medical Research Institue, Surgical Research Branch, Combat Casualty Research Program Center, Bethesda, MD; AE McKee Principal Investigator.

6.1 Grant--Pathophysiology of Septic Shock ($100,000/yr for 3 years) 6.3 Grant--Treatment of Septic Shock ($500,000-600,000/yr for 5 years)

1989-91 Dana Foundation Fellowship in the Neurosciences, Department of Psychiatry, Stanford University Medical Center, Stanford, CA.

"Molecular mechanisms of serotonin receptor regulation" $35,800/yr for 2 years BL Roth MD, PhD Recipient RD Ciaranello MD Faculty Advisor

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1991-1993 Pharmaceutical Manufacturers Starter Research Grant Award, Department of Psychiatry, Case Western Reserve University School of Medicine, Cleveland, OH.

"Molecular and biochemical mechanisms of 5HT2 receptor regulation" $10,000/yr for 2 years BL Roth MD, PhD Principal Investigator

1991-1993 Scottish Rite Schizophrenia Research Award, Department of Psychiatry, Case Western Reserve University School of Medicine, Cleveland, OH.

"Interaction of typical and atypical antipsychotic agents with chimeric serotonin receptors"

$30,000/yr for 2 years (plus 15% indirect costs) BL Roth MD, PhD Principal Investigator

1992-1994 NARSAD Award, Department of Psychiatry, Case Western Reserve University School of Medicine, Cleveland, OH.

"Molecular mechanisms of clozapine action" $30,000/ yr for 2 years BL Roth MD, PHD Principal Investigator.

1992-1997, MHCRC on Major Psychotic Disorders (NIMH), Department of Psychiatry, Case Western Reserve University School of Medicine, Cleveland, OH.

$765,000/year (direct costs/year; 5 years) Herbert Y. Meltzer, Principal Investigator BL Roth MD,PhD Co-Investigator

Core #9 -- Atypical Antipsychotic Drug Action 10% Effort

1993-94 Effects of F340L mutation on drug binding $3,000, Department of Psychiatry, Case Western Reserve University School of Medicine, Cleveland, OH. BL Roth MD, PhD Principal Contractor 1994-1997 1RO1GM52213-01, Department of Psychiatry, Case Western Reserve University School of Medicine, Cleveland, OH.

"Structural domains responsible for serotonin receptor pharmacology." $608,043 (3 years; total costs) BL Roth MD, PhD Principal Investigator 7/1/94 - 6/30/97 35% Effort

1996-2001 KO2MH001366, Department of Biochemistry, Case Western Reserve University School of Medicine, Cleveland, OH. “Molecular mechanisms of 5-HT receptor actions” $502,250 (5 years, total costs) BL Roth MD, PhD, Principal Investigator 7/1/96-6/30/01 1997-2001 RO1 MH 57635-04 Department of Biochemistry, Case Western Reserve University

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School of Medicine, Cleveland, OH. “Structural domains responsible for serotonin receptor pharmacology” $898,305 BL Roth MD, PhD Principal Investigator 7/1/97-6/30/01 1998-2003 NO1MH80005 NIMH Department of Biochemistry, Case Western Reserve University School of Medicine, Cleveland, OH. ‘NIMH Psychoactive Drug Screening Program’ $4,561,270 BL Roth MD, PhD, Principal Investigator 9/30/98 – 9/30/03 1998-1999 NARSAD Independent Investigator Award, Department of Biochemistry ‘Targeting of 5-HT2A receptors to apical dendrites’ $98,200 BL Roth MD, PhD Principal Investigator 9/15/98-9/14/00 (In no-cost extension) 1998 SK Corporation Grant-in-Aid: Effect of YKP10A on biogenic amine receptors: in vivo and in vitro studies. $34,500 Effort: N/A BL Roth MD, Ph.D., Principal Investigator 2001-2003 NARSAD Young Investigator Award Alteration of Gene Expression in Antipsychotic Drug Treated Cells Department of Biochemistry, Case Western Reserve University Medical School, Cleveland, OH. WK Kroeze, PI 50% Effort $58,000 2003-2005 R43 DK065322 Psilocybin Analogues As Novel Pharmacologic Agents Subcontract with Organix, Inc. Boston,MA

BL Roth PI (on subcontract) 5% effort $84,000

2001-2008 RO1MH57635-04 (NIMH). Structural Domains Essential For Serotonin Receptor Pharmacology UNC Chapel Hill Medical School.

BL Roth, PI 20% Effort $1,539,299

2002-2004 American Heart Association 0215080B Molecular and Cellular Mechanisms of Fenfluramine-Induced Valyulopathy Department of Biochemistry, Case Western Reserve University Medical School, Cleveland, OH.

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Vincent Setola, PI 90% Effort $34,000 2002-2004 F31 MH067435 The Interaction if RSK2 with the 5HT2A Receptor Department of Biochemistry, Case Western Reserve University Medical School, Cleveland, OH. Douglas Sheffler, PI 90% Effort $68,150 1996-2001 KO2 MH01366 RSDA Type II (NIMH). Molecular Mechanisms Of 5HT Receptor Actions Departments of Biochemistry and Psychiatry, Case Western Reserve University School of Medicine, Cleveland, OH.

BL Roth MD, PHD, Principal Investigator 75% Effort (Salary support for all research efforts) $495,960

2001-2005 MH60599, Design And Synthesis Of 5-HT6 Selective Serotonergic Agents Subcontract Medical College of Virginia BL Roth PI (on subcontract) 5% Effort $ 338,800 2001-2006 KO2 MH01366 RSDA Type II (NIMH). Molecular Mechanisms Of 5HT Receptor Actions Departments of Biochemistry, Case Western Reserve University School of Medicine, Cleveland, OH.

BL Roth, PI 75% Effort (Salary support for all research efforts) $592,920

National Research Service Award Creation of Designer Biogenic Amine Receptor Department of Biochemistry, Case Western Reserve University Medical School, Cleveland, OH. Timothy Vortherms, PI 90% Effort

$92,272 2005-2007 F32GM074554 Creation of Designer Biogenic Amine Receptor Department of Biochemistry, Case Western Reserve University Medical School, Cleveland, OH. Blaine Armbruster, PI 90% Effort $98,244 2004-2006 NARSAD Young Investigator Award Relationship Between Binding of Atypical Antipsychotics to GPCR’s and Propensity to Induce Weight Gain Department of Biochemistry, Case Western Reserve University Medical School, Cleveland, OH. WK Kroeze, PI 50% Effort

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$60,000 2003-2008 NO1MH32004 NIMH Psychoactive Drug Screening Program Contract (NIMH); continuation of NO1MH80002 Department of Biochemistry, Case Western Reserve University School of Medicine, Cleveland,OH BL Roth, PI 30% Effort $8, 675,125 2006-2009 Continuation of: R43 DK065322 Psilocybin Analogues As Novel Pharmacologic Agents Subcontract with Organix, Inc. Boston,MA BL Roth PI (on subcontract) 5% Effort

$314,613

2003-2008 RO1DA017204-06 Diterpines As Kappa Opioid Agonists, UNC Chapel Hill Medical School BL Roth, PI 15% Effort $1,515,000 2008-2010 NARSAD Distinguished Investigator Award. UNC Chapel Hill Medical School BL Roth, PI 0% Effort $100,000 2006-2010 RO1MH46851 Design and Synthesis of Anxioselective Anxiolytics Subcontract with University of Wisconsin-Milwaukee UNC Chapel Hill Medical School BL Roth, PI 5% Effort $180,000 2009-2011 RO1DA022317 Chemistry and Biology of 5-HT2C Receptors for Drug AbuseS UNC Chapel Hill Medical School Subcontract with University of Chicago NIH/NIDA Kozikowski , PI 1% effort $233,566 2009-2011(None) Angelman Syndrome Foundation Novel Therapeutics for Angelman Syndrome by Manipulating Ube3a Expression UNC Chapel Hill Medical School Philpot, PI BL Roth, Co-PI 2% Effort $90,909 2009-2012 F30MH087074 In Vivo Neuronal Modulation via Engineered G-Protein Coupled Receptors UNC Chapel Hill Medical School Rogan, PI

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90% Effort NIH/NIMH $83,121 2008-2013: NIMH Psychoactive Drug Screening Program Contract BL Roth PI $10,000,000 (approximate) 2009 -2013 RO1DA027170-01 Deorphanizing the Peptidome UNC Chapel Hill Medical School Iris Lindberg, University of Maryland, BL Roth Co-PI’s $1,207,000 2011-2013: Small molecule therapeutics for autism. UNC Chapel Hill Medical School. Simons Foundation Philpot, PI BL Roth, Co-PI $1,000,030 (approximate) 2010-2015 RO1MH61887-11. Regulation Of 5-HT2A Receptor Trafficking Department of Biochemistry, UNC Chapel Hill Medical School.

BL Roth, PI 15% Effort $1, 250,000 (Direct)

2010-2015 RO1DA017204-06 Diterpines As Kappa Opioid Agonists, UNC Chapel Hill Medical School BL Roth, PI 15% Effort $1,515,000 2013-2015: Small molecule therapeutics for Rett Sydrome. UNC Chapel Hill Medical School. RSF. BL Roth, T Magnusson and B Philpot Co-PI’s $2,200,000 (approximate) 2014-2017: U01MH104974-01: Scalable technologies for illuminating the druggable GPCR-ome, UNC Chapel Hill Medical School BL Roth and B Shoichet Co-PI $1,200,000 (approximate total award) 2014-2017: UO1MH105892: DREADD2.0: an enhanced chemogenetic toolkit. UNC Chapel Hill BL Roth, T Kash and J Jian Co-PI’s $2,850,000 (approximate total award) 2012-2017 U19MH082441 Functional selectivity: a novel approach for CNS drug discovery. UNC Chapel Hill Medical School

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BL Roth, PI 10% Effort $8,000,000 (approximate total award) 2012-2017: RO1MH099653: Optimizing lead 5-HT2C ligands for use in the treatment of schizophrenia A Kozikowski and BL Roth (MPI) $3, 300,000 (approximate total)