TheJournalof PHARMACOLOGY · Rather than Alpha Adrenergic Receptors Comparison of the Response to...

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TheJournalof VOLUME253 PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS Contents ANALGESICS Dissociation of Mu Opioid Tolerance from Receptor Down- Kyoko Nishino. Y. F. Su, C.-S. Wong, 67 Regulation in Rat Spinal Cord W. D. Watkins and K.-J. Chang AUTONOMIC PHARMACOLOGY Pharmacological Differentiation of Angiotensin Effects in the George J. Trachte 80 Rabbit Isolated Vas Deferens with Dithiothreitol and Pertussis Toxin Functional Determination of McN-A-343 Affinity for M1 R. Micheletti and A. Schiavone 310 Muscarinic Receptors BEHAVIORAL PHARMACOLOGY Effect of Phenylpiperidine Opioid Antagonists on Food Walter N. Shaw, Charles H. Mitch. J. 85 Consumption and Weight Gain of the Obese Zucker Rat David Leander and Dennis M. Zimmerman CARDIOVASCULAR PHARMACOLOGY On the Mechanism of the Different Sensitivity of Purkinje Giovanni lacono and Mario Vassalle I and Myocardial Fibers to Strophanthidin Endothelial Nitric Oxide Generating Enzyme(s) in the Bovine Kathleen M. Boje and Ho-Leung Fung 20 Aorta: Subcellular Location and Metabolic Characterization Antagonism of Leukotriene B4 Receptors Does Not Limit Richard A. Hahn, Brian R. MacDonald. 58 Canine Myocardial Infarct Size Paul J. Simpson, Brian D. Potts and C. John Parli Age-Dependent Baroreflex Attenuation by Centrally Infused Donna L. Bamnger and Ruben D. 158 Verapamil in Rats Bu#{241}ag Cardiac Dysfunction Caused by Recombinant Human C5A Ughetta del Baizo, Ichiro Sakuma and 171 Anaphylatoxin: Mediation by Histamine, Adenosine and Roberto Levi Cyclooxygenase Arachidonate Metabolites Different Patterns of Autonomic Nerve Activity Produced by a Winona R. Rebagay and Robert W. 180 Polar vs. a Neutral Cardiac Glycoside Caldwell Inotropic, Electrophysiological and Biochemical Responses to Yuichi Hattori, Haruaki Nakaya, 250 Histamine in Rabbit Papillary Muscles: Evidence for Masayuki Endou and Mono Kanno Coexistence of H1- and H2-Receptors Comparison between the Vasoactive Actions of Endothelin Reza Tabrizchi and Christopher R. 272 and Arginine Vasopressin in Pithed Rats after Pretreatment Triggle with BAY K 8644, Nifedipine or Pertussis Toxin Calcium Antagonists Show Two Modes of Protection in Frank Th. M. van Amsterdam, Nieko C. 277 Ischemic Heart Failure Punt, Marijke Haas and Johan Zaagsma Inotropic and Lusitropic Effects of Chlorpromazine on Rat Michel Clergue, Bruno Riou and Yves 296 Left Ventricular Papillary Muscle Lecarpentier Autonomic Modulation of the Frequency-Dependent Actions Mohsen Nayebpour, Mario Talajic, 353 of Diltiazem on the Atrioventricular Node in Anesthetized Wuhua Jing and Stanley Nattel Dogs Alpha Adrenoceptor Activation and Postreceptor Contractile M. J. Stevens and R. F. W. Moulds 375 Mechanisms in the Human Digital Artery CELLULAR AND MOLECULAR PHARMACOLOGY Activation of Protein Kinase C Inhibits Internalization and Randall K. Hoover and Myron L. 185 Downregulation of Muscarinic Receptors in 1321 NI Human Toews Astrocytoma Cells (‘onu’n!s continued on iv at ASPET Journals on December 10, 2020 jpet.aspetjournals.org Downloaded from

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Page 1: TheJournalof PHARMACOLOGY · Rather than Alpha Adrenergic Receptors Comparison of the Response to 5-Carboxamido tryptamine Noboru Toda and Tomio Okamura 676 and Serotonin in Isolated

The Journalof

VOLUME253 PHARMACOLOGY� AND EXPERIMENTAL THERAPEUTICS

Contents

ANALGESICS

Dissociation of Mu Opioid Tolerance from Receptor Down- Kyoko Nishino. Y. F. Su, C.-S. Wong, 67

Regulation in Rat Spinal Cord W. D. Watkins and K.-J. Chang

AUTONOMIC PHARMACOLOGY

Pharmacological Differentiation of Angiotensin Effects in the George J. Trachte 80Rabbit Isolated Vas Deferens with Dithiothreitol and

Pertussis Toxin

Functional Determination of McN-A-343 Affinity for M1 R. Micheletti and A. Schiavone 310

Muscarinic Receptors

BEHAVIORAL PHARMACOLOGY

Effect of Phenylpiperidine Opioid Antagonists on Food Walter N. Shaw, Charles H. Mitch. J. 85Consumption and Weight Gain of the Obese Zucker Rat David Leander and Dennis M.

Zimmerman

CARDIOVASCULAR PHARMACOLOGY

On the Mechanism of the Different Sensitivity of Purkinje Giovanni lacono and Mario Vassalle Iand Myocardial Fibers to Strophanthidin

Endothelial Nitric Oxide Generating Enzyme(s) in the Bovine Kathleen M. Boje and Ho-Leung Fung 20

Aorta: Subcellular Location and Metabolic Characterization

Antagonism of Leukotriene B4 Receptors Does Not Limit Richard A. Hahn, Brian R. MacDonald. 58Canine Myocardial Infarct Size Paul J. Simpson, Brian D. Potts and C.

John Parli

Age-Dependent Baroreflex Attenuation by Centrally Infused Donna L. Bamnger and Ruben D. 158

Verapamil in Rats Bu#{241}ag

Cardiac Dysfunction Caused by Recombinant Human C5A Ughetta del Baizo, Ichiro Sakuma and 171Anaphylatoxin: Mediation by Histamine, Adenosine and Roberto LeviCyclooxygenase Arachidonate Metabolites

Different Patterns of Autonomic Nerve Activity Produced by a Winona R. Rebagay and Robert W. 180Polar vs. a Neutral Cardiac Glycoside Caldwell

Inotropic, Electrophysiological and Biochemical Responses to Yuichi Hattori, Haruaki Nakaya, 250Histamine in Rabbit Papillary Muscles: Evidence for Masayuki Endou and Mono Kanno

Coexistence of H1- and H2-Receptors

Comparison between the Vasoactive Actions of Endothelin Reza Tabrizchi and Christopher R. 272

and Arginine Vasopressin in Pithed Rats after Pretreatment Triggle

with BAY K 8644, Nifedipine or Pertussis Toxin

Calcium Antagonists Show Two Modes of Protection in Frank Th. M. van Amsterdam, Nieko C. 277Ischemic Heart Failure Punt, Marijke Haas and Johan Zaagsma

Inotropic and Lusitropic Effects of Chlorpromazine on Rat Michel Clergue, Bruno Riou and Yves 296

Left Ventricular Papillary Muscle Lecarpentier

Autonomic Modulation of the Frequency-Dependent Actions Mohsen Nayebpour, Mario Talajic, 353

of Diltiazem on the Atrioventricular Node in Anesthetized Wuhua Jing and Stanley Nattel

Dogs

Alpha Adrenoceptor Activation and Postreceptor Contractile M. J. Stevens and R. F. W. Moulds 375

Mechanisms in the Human Digital Artery

CELLULAR AND MOLECULAR PHARMACOLOGY

Activation of Protein Kinase C Inhibits Internalization and Randall K. Hoover and Myron L. 185Downregulation of Muscarinic Receptors in 1321 NI Human ToewsAstrocytoma Cells

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Subtype-Selective Regulation of Beta Adrenergic Receptor- Marian T. Nakada, Jeffrey M. Stadel 221Adenylyl Cyclase Coupling by Phorbol Esters in 3T3-LI and Stanley T. Crooke

Fibroblasts

Cross-Linking of Human f’251jfi-Endorphin to Opioid Anton N. M. Schoffelmeer, Yi-He Yao, 419Receptors in Rat Striatal Membranes: Biochemical Evidence Theresa L. Gioannini, Jacob M. Hiller,

for the Existence of a mu/delta Opioid Receptor Complex Danielle Ofri, Bernard P. Roques and

Eric J. Simon

DEVELOPMENTAL PHARMACOLOGY

Effects of Sympathetic Activation on Plasma Renin Activity in Robert F. Kirby and Alan Kim Johnson 152

the Developing Rat

Maternal Age and Blood Alcohol Concentration in the Michael W. Church, Ernest L. Abel, 192

Pregnant Long-Evans Rat Barbara A. Dintcheff and Carol

Matyjasik

DRUG METABOLISM AND DISPOSITION

Effects of Protein Binding and Experimental Disease States Tsu-Han Lin and Jiunn H. Lin 45

on Brain Uptake of Benzodiazepines in Rats

Uptake Kinetics of 2’,3’-Dideoxyinosine into Brain and Bradley D. Anderson, Barbara L. 1 13Cerebrospinal Fluid of Rats: Intravenous Infusion Studies Hoesterey, David C. Baker and

Raymond E. Galinsky

Effects of Plasma Protein Binding Displacement on the Bruce J. Aungst, Judy A. Blake, Nancy 230Pharmacokinetics, Tissue and Tumor Concentrations and J. Rogers and Betsy A. Dusak

Efficacy of Brequinar, a Highly Protein-Bound Antitumor

Agent

Assessment of Cyclosporine A Interactions with Human S. Urien, R. Zini, M. Lemaire and J. P. 305

Plasma Lipoproteins in Vitro and in Vivo in the Rat Tillement

In Vivo Evidence for Carrier-Mediated Uptake of fl-Lactam Akira Tsuji, Tetsuya Terasaki, Ikumi 315Antibiotics through Organic Anion Transport Systems in Rat Tamai and Kazuyoshi Takeda

Kidney and Liver

Alteration of Plasma Sex Hormone Levels Associated with Shoichi Fujita, Masato Chiba, Minoru 369

Old Age and Its Effect on Hepatic Drug Metabolism in Rats Ohta, Kenichi Kitani and Tokuji Suzuki

ENDOCRINE PHARMACOLOGY

Differential Regulation of Heme and Drug Metabolism in Rat MUmtaz Iscan and Mahin D. Maines 73Testis and Prostate: Response to cis-Platinum and HumanChorionic Gonadotropin

GASTROINTESTINAL PHARMACOLOGY

Opioid Regulation of Mucosal Ion Transport in the Mouse Russell J. Sheldon, Pierre J. M. Rivi#{232}re, 144Isolated Jejunum Margaret E. Malarchik, Henry I.

Mosberg, Thomas F. Burks and FrankPorreca

fTyr#{176}1-Calcitonin Gene-Related Peptide 28-37 (Rat) as a Sushanta Chakder and Satish Rattan 200Putative Antagonist of Calcitonin Gene-Related PeptideResponses on Opossum Internal Anal Sphincter SmoothMuscle

NEUROPHARMACOLOGY

Interaction of Amitriptyline, Doxepin, Imipramine and Their Frederick J. Ehlert, Frank M. Delen, 13N-Methyl Quaternary Ammonium Derivatives with Subtypes Susan H. Yun and Henny A. Liem

of Muscarinic Receptors in Brain and Heart

Heterogeneity of High-Affinity Nicotinic �3HJAcetylcholine Ronald J. Lukas 51

Binding Sites

Electrophysiological Evidence that Ethanol Alters Function of Bennet S. Givens and George R. Breese 95

Medial Septal Area without Affecting Lateral Septal Function

Effects of Repeated Fenfluramine Administration on Indices Robert Zaczek, George Battaglia, Steven 104

of Monoamine Function in Rat Brain: Pharmacokinetic, Dose Culp, Nathan M. Appel, Joseph F.Response, Regional Specificity and Time Course Data Contrera and Errol B. De Souza

Multiple Vascular Effects of Sigma and PCP Ligands: Tania Massamiri and Sue Piper Duckles 124

Inhibition of Amine Uptake and Contractile Responses

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Contents continuedjrom iv

Competitive and Noncompetitive N-Methyl-L-Aspartate John J. Grigg and Edmund G. Anderson I 30Antagonists Modify Hypoxia-Induced Membrane Potential

Changes and Protect Rat Hippocampal Slices from Functional

Failure: A Quantitative Comparison

Centrally Active Antimuscarinic Analogs of Oxotremorine Hugo M. Vargas and Bj#{246}rnRingdahl 165Selectively Block Physostigmine-Induced Hypertension, but

not Peripheral Muscarinic Vasodepression

Characterization of Dl Dopamine Receptors in the Bovine V. Simonneaux, L. C. Murrin and M. 214Pineal Gland with I3HISCH 23390 Ebadi

Molecular Mechanisms of Homologous Desensitization and Carola Eva, Silvana Ricci Gamalero, 257Internalization of Muscarinic Receptors in Primary Cultures Enrico Genazzani and Erminio Costaof Neonatal Corticostriatal Neurons

Eltoprazine Suppresses Hyperpolarizing Responses to M. Jo#{235}ls,C. M. A. Pennartz, H. 284

Serotonin in Rat Hippocampus Sijbesma and J. Schipper

Adenosine Receptors are Coupled Negatively to Release of F. L. Christofi, T. J. McDonald and M. 290

Tachykinin(s) from Enteric Nerve Endings A. Cook

Abecarnil, a Metabolically Stable, Anxioselective fl-Carboline D. N. Stephens, H. H. Schneider, W. 334Acting at Benzodiazepine Receptors Kehr, J. S. Andrews, K.-J. Rettig, L.

Turski, R. Schmiechen, J. D. Turner, L.H. Jensen, E. N. Petersen, T. Honore

and J. Bondo Hansen

Anticonvulsant Action of the $-Carboline Abecarnil: Studies L. Turski, D. N. Stephens. L. H. Jensen, 344in Rodents and Baboon, Papio papio E. N. Petersen, B. S. Meldrum, S. Patel,

J. Bondo Hansen, W. LOscher, H. H.Schneider and R. Schmiechen

Attenuation of Opioid Receptor Activity by Phorbol Esters in Alan K. Louie, Evan S. Bass. Junni 401

Neuroblastoma x Glioma NG1O8-15 Hybrid Cells Zhan, Ping Yee Law and Horace H. Loh

Role of Imidazole Receptors in the Vasodepressor Response Paul Ernsberger, Rachel Giuliano. 408

to Clonidine Analogs in the Rostral Ventrolateral Medulla Robert N. Willette and Donald J. Reis

PHARMACOLOGY OF SUBSTANCE ABUSE

Persistence of Neurochemical Changes in Dopamine Systems Joanna Pens, Sally J. Boyson, Wayne A. 38After Repeated Cocaine Administration Cass, Pamela Curella, Linda P.

Dwoskin, Gaynor Larson, Lie-Huey Lin,Robert P. Yasuda and Nancy R.Zahniser

Operant Acquisition of Alcohol by Women Nancy K. Mello, Jack H. Mendelson, 237Susan Palmieri, Barbara W. Lex and

Siew K. Teoh

PROSTAGLANDINS AND LEUKOTRIENES

Contrasting Effect of Thromboxane Synthase Inhibitors and a Mahesh Mistry and Alberto Nasjletti 90Thromboxane Receptor Antagonist on the Development ofAngiotensin Il-Salt-Induced Hypertension in Rats

Chronic Treatment with Propranolol Enhances the Synthesis Takatoshi Nishimiya, Herman B. 207

of Prostaglandins E2 and 12 by the Aorta of Spontaneously Daniell, Jerry G. Webb, John Oatis,Hypertensive Rats Thomas Walle, Thomas E. Gaffney and

Perry V. Halushka

PULMONARY PHARMACOLOGY

Histamine and Methacholine Aerosol Bronchial Challenge in Mildred J. Wiester, Jeffrey S. Tepper. 27Awake Guinea Pigs Mary F. Weber and Margaret G.

M#{232}nache

Distribution of Substance P Receptors in Rabbit Airways, Judith Black, Leonie Diment. Carol 381Functional and Autoradiographic Studies Armour, Lorraine Alouan and Peter

Johnson

RENAL PHARMACOLOGY

Mechanisms of Amphotericin B-Induced Reduction of the Ramzi Sabra, Kihito Takahashi, Robert 34

Glomerular Filtration Rate: A Micropuncture Study A. Branch and Kamal F. Badr

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Effect of Enalapril or the Thromboxane Receptor Antagonist, David P. Brooks, Lisa C. Contino, 1 19Daltroban, in Rats With Subtotal Renal Ablation Walter Trizna, Richard M. Edwards,

Eliot H. Ohistein and Henk A. Solleveld

Pharmacological Characterization of Rat Renal Medulla Francesco Amenta, Alberto Ricci and 246

Dopamine-Sensitive Cyclic Adenosine Monophosphate Jos#{233}A. VegaGenerating System

Contribution of Renal Nerves to the Natriuretic and Diuretic R. L. Kline and P. F. Mercer 266Effect of Alpha-2 Adrenergic Receptor Activation

Platelet-Activating Factor Antagonists Treatment Protects Antonio L#{244}pez-Farr#{232},Fernando 328against Postischemic Acute Renal Failure in Rats Bernabeu, Dulcenombre G#{244}mez-Garre,

Santiago Ramon y Cajal, Pierre Braquetand Jos#{233}M. L#{244}pez-Novoa

Pharmacokinetic and Pharmacodynamic Actions of Enalapril Faruq H. Noormohamed, W. Robin 362

in Humans: Effect of Probenecid Pretreatment McNabb and Ariel F. Lant

TOXICOLOGY

Effects of Dose, Age, Inhibition of Metabolism and Burhan I. Ghanayem. J. M. Sanders, 136Elimination on the Toxicokinetics of 2-Butoxyethanol and Its Ann-Marie Clark, John Bailer and H. B.Metabolites Matthews

Effect of Lithium on Renal Transport and Utilization of a- Bernard Ferrier. Mireille Martin and 321Ketoglutarate in the Rat Gabriel Baverel

Cytochrome P 450 Isoenzymes, Epoxide Hydrolase and I. de Waziers, P. H. Cugnenc, C. S. 387#{149}Glutathione Transferases in Rat and Human Hepatic and Yang, J.-P. Leroux and P. H. Beaune

Extrahepatic Tissues

Muscarine Depolarizes Rat Substantia Nigra Zona Compacta M. G. Lacey, P. Calabresi and R. A. 395and Ventral Tegmental Neurons in Vitro Through M,-Like NorthReceptors

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The Journal of

VOLUME253 PHARMACOLOGY��02 AND EXPERIMENTAL THERAPEUTICS

Contents

AUTONOMIC PHARMACOLOGY

Adenosine Receptor Antagonism Attenuates Angiotensin II George J. Trachte and Lois J. Heller 490

Effects on Adrenergic Neurotransmission in the Rabbit

Isolated Vas Deferens

Effect of Protein Kinase C Inhibitors on the Actions of E. Sehic and K. U. Malik 497

Phorbol Esters on Vascular Tone and AdrenergicTransmission in the Isolated Rat Kidney

Characterization of Vascular Muscarinic Receptors: Rabbit Sue Piper Duckles and 608Ear Artery and Bovine Coronary Artery Angel Luis Garcia-Villalon

Autonomic Receptors in Urinary Tract: Sex and Age Jamshid Latifpour. Shun Kondo. 661Differences Brian O’Hollaren, Takashi Morita and

Robert M. Weiss

BEHAVIORAL PHARMACOLOGY

Effects of Cholecystokinin, d-Amphetamine and Fenfluramine Rebecca L. Corwin. 720in Rats Trained to Discriminate 3 from 22 Hr of Food William L. Woolverton andDeprivation Charles R. Schuster

Effects of Desipramine Maintenance on Cocaine Self- Marian W. Fischman, 760Administration by Humans Richard W. Foltin, Gerald Nestadt and

Godfrey D. Pearlson

CARDIOVASCULAR PHARMACOLOGY

Central Sympathoinhibitory Action of a New Type of Alpha-l Mitsuhiro Yoshioka, Hiroko Togashi, 427Adrenoceptor Antagonist, YM-617, in Rats Masayuki Abe, Toshiya Ikeda,

Machiko Matsumoto and Hideya Saito

Failure of Propranolol to Inhibit the Epinephrine-Induced Patrick H. J. Falckh. Ivan S. de la Lande, 432Enhancement of Responses to Sympathetic Nerve Stimulation Robert E. Stitzel, Mark Mano andin the Rat Mesenteric Vascular Bed Richard J. Head

Similarities in the Pharmacological Modulation of Reactive Michael S. Wolin, Jean M. Rodenburg, 508

Hyperemia and Vasodilation to Hydrogen Peroxide in Rat Edward J. Messina and Gabor KaleySkeletal Muscle Arterioles: Effects of Probes forEndothelium-Derived Mediators

Evaluation of a Potent Inhibitor of Subprimate and Primate J. M. Wood, S. C. Mah, H. P. Baum. 513Renins M. de Gasparo. F. Cumin. H. RUeger

and J. Nussberger

Beta Adrenoceptor Subtype in Isolated Human, Monkey and Noboru Toda and Tomio Okamura 518Dog Epicardial Coronary Arteries

Protective Effects of the Specific Thromboxane Receptor Louis E. Furlan, Gerald Johnson III, 525

Antagonist (+)-S145Na in Splanchnic Artery Occlusion Martin Siegfried and Allan M. LeferShock in Rats

Influence of Amiloride Derivatives on Alpha-i Adrenergic Charles Lesburg. Shauna Li, 530Receptor-Induced Contractions of the Rabbit Aorta Edward J. Cragoe, Jr. and

Richard C. Deth

Effects of an Aldose Reductase Inhibitor, ONO-2235, Insulin Hisakuni Hashimoto, Natsuki Satoh, 552and Their Combination on the Altered Responsiveness to the Yoshiharu Takiguchi andNerve Stimulation and Agonists of the Isolated Atria of Mitsuyoshi NakashimaDiabetic Rats

Comparison of Effects of Cromakalim and Pinacidil on Kaoru Masuzawa, Masahisa Asano, 586Mechanical Activity and �Rb Efflux in Dog Coronary Tomohiro Matsuda. Yuji Imaizumi andArteries Minoru Watanabe

Identification of the Subcellular Site for Nitroglycerin Suk-Jae Chung and Ho-Leung Fung 614Metabolism to Nitric Oxide in Bovine Coronary SmoothMuscle Cells

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Protection Against Hypoxic Injury in Isolated-Perfused Rat Youngja Park, Douglas K. Bowles and 628Heart by Ruthenium Red James P. Kehrer

Differentiated Response of Renal and Adrenal Sympathetic Martin Delle, Peter Thor#{233}n, 655Nerve Activity to Intravenous Morphine Administration in Jon 0. Skarphedinsson. Pavel Hoffman,Anesthetized Rats Stefan Carlsson and Sven-Erik Ricksten

Effect of Ouabain on the Rabbit Ear Artery Contraction to Z. Xu, G. Mondal, J. P. Song and 668Serotonin: Enhanced Response Mediated by Serotonergic R. E. PurdyRather than Alpha Adrenergic Receptors

Comparison of the Response to 5-Carboxamido tryptamine Noboru Toda and Tomio Okamura 676and Serotonin in Isolated Human, Monkey and Dog CoronaryArteries

Inhibitory Effects of Amiloride on Alpha Adrenoceptors in A. G. Shi, Z. L. Wang, C. Y. Kwan and 791

Canine Vascular Smooth Muscle E. E. Daniel

Activity of the Short-Acting Thromboxane Receptor William A. Schumacher, 841Antagonist, SQ 30,741, in Thrombolytic and Vasospastic Christopher L. Heran, Karen S. HartlModels in Monkeys and Martin L. Ogletree

Species Differences in Chlorethylclonidine Antagonism at Wang-Ni Tian, Sandeep Gupta and 877Vascular Alpha-I Adrenergic Receptors Richard C. Deth

CELLULAR AND MOLECULAR PHARMACOLOGY

I3HITA-3090, a Selective Benzothiazepine-type Calcium Ray H. Zobrist and Thomas E. Mecca 461Channel Receptor Antagonist: In Vitro Characterization

Tocolytic Agents Act on Calcium Channel Current in Single Yusuke Ohya and Nicholas Sperelakis 580Smooth Muscle Cells of Pregnant Rat Uterus

Receptor-Coupled Signal Transduction in Human Robert J. Smith, Laurel M. Sam, 688Polymorphonuclear Neutrophils: Effects of a Novel Inhibitor James M. Justen, Gordon L. Bundy,of Phospholipase C-Dependent Processes on Cell Gregory A. Bala and John E. BleasdaleResponsiveness

Alterations by Glyburide of Effects of BRL 34915 and P 1060 Shiling Hu, Helen S. Kim, 771

on Contraction, �‘Rb Efflux and the Maxi-K� Channel in Rat Patience Okolie and George B. Weiss� Portal Vein

I3Hlldazoxan Binding to the Ovine Myometrium. Binding Anne Vass-Lopez. R. Garcia-Villar. 819

Characteristics and Changes due to Steroid Hormones M. Lafontan and P. L. Toutain

Effects of a Choline-Deficient Ethionine-Supplemented Diet U. Leli, A. Saluja. L. Picard. 847

on Phospholipase C Activity in Mouse Pancreatic Acinar Cell A. Zavertnik and M. L. SteerMembranes and in Electropermeabilized Mouse PancreaticAcini

DRUG METABOLISM AND DISPOSITION

Membrane Potential-Dependent and Carrier-Mediated Ikumi Tamai. Tatsuyuki Maekawa and 537Transport of Cefpiramide, a Cephalosporin Antibiotic, in Akira TsujiCanalicular Rat Liver Plasma Membrane Vesicles

ENDOCRINE PHARMACOLOGY

Effects of Peripheral Benzodiazepine Receptor Ligands on Aldo E. Calogero, Themis C. Kamilaris. 729Hypothalamic-Pituitary-Adrenal Axis Function in the Rat Renato Bernardini,

Elizabeth 0. Johnson.

George P. Chrousos and Philip W. Gold

GASTROINTESTINAL PHARMACOLOGY

Age-Related Changes in Enteric Neuromuscular Transmission Thomas V. Nowak, Bonnie Hamngton 683and John Kalbfleisch

Vasoactive Intestinal Peptide (VIP) as Transmitter of J. R. Grider and J. R. Rivier 738Inhibitory Motor Neurons of the Gut: Evidence from the Useof Selective VIP Antagonists and VIP Antiserum

Effects of Bombesin on Mucosal Ion Transport in the Mouse Pierre J. M. Rivi#{232}re,Russell J. Sheldon. 778Isolated Jejunum Margaret E. Malarchik. Thomas F. Burks

and Frank Porreca

Opioid Modulation of Basal Intestinal Fluid Transport in the Qi Jiang, Russell J. Sheldon and 784

Mouse: Actions at Central, but not Intestinal, Sites Frank Porreca

Regulation of Serotonin Release from Enterochromaffin Cells C. Simon and J. P. Ternaux 825of Rat Cecum Mucosa

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NEUROPHARMACOLOGY

Ifenprodil and SL 82.0715 as Cerebral Antiischaemic Agents. Christopher J. Carter. Kenneth G. Lloyd. 475III. Evidence for Antagonistic Effects at the Polyamine Branimir Zivkovic and Bernard ScattonModulatory Site Within the N-Methyl-o-Aspartate

Opioid-Induced Epileptiform Bursting in Hippocampal Slices: Paul H. K. Lee, Cui-Wei Xie, 545Higher Susceptibility in Ventral than Dorsal Hippocampus Darrell V. Lewis, Wilkie A. Wilson.

Clifford L. Mitchell and Jau-

Shyong Hong

Functional Modulation of Cerebral ‘y-Aminobutyric AcidA Jun-Ichi Taguchi and Kinya Kunyama 558Receptor/Benzodiazepine Receptor/Chloride Ion ChannelComplex with Ethyl �9-Carboline-3-Carboxylate: Presence ofIndependent Binding Site for Ethyl fl-Carboline-3-Carboxylate

Characterization of Cholinergic Muscarinic Receptor- Walter Balduini. Sheldon D. Murphy 573Stimulated Phosphoinositide Metabolism in Brain from and Lucio G. CostaImmature Rats

Behavioral Changes Induced by Stressful Situations: Effects Akira Katoh, Toshitaka Nabeshima and 600of Enkephalins, Dynorphin, and Their Interactions Tsutomu Kameyama

Effect of Ouabain on the i’-(3HlAminobutyric Acid Uptake M. S. Santos, P. P. Gon#{231}alves and 620and Release in the Absence of Ca� and K�-Depolarization A. P. Carvalho

Cyclazocine and Pentazocine as N-Methylaspartate John Church and David Lodge 636Antagonists on Cat and Rat Spinal Neurons in Vivo

Antinociceptive Effects of Intrathecal Adrenoceptor Agonists R. M. Danzebrink and G. F. Gebhart 698in a Rat Model of Visceral Nociception

Characterization of Kappa Opioid Binding Using Dynorphin Thomas Devlin and 749A11,� and U69,593 in the Rat Brain William J. Shoemaker

Serotonergic Afferent Regulation of the Basic Physiology and Mark D. Kelland. Arthur S. Freeman 803Pharmacological Responsiveness of Nigrostriatal Dopamine and Louis A. ChiodoNeurons

Rapid Desensitization of Dopamine Release Induced by Barbara M. Faggin and 812

Neurotensin and Neurotensin Fragments Luigi X. Cubeddu

Antidepressant Actions on Brain Noradrenergic Neurons Rita J. Valentino, Andre L. Curtis, 833

Dana G. Pams and Richard G. Wehby

Neuropeptide Processing in Regional Brain Slices: Effect of Z. W. Li, W. A. A. J. Bijl. 851Conformation and Sequence J. W. van Nispen, K. Brendel and

T. P. Davis

Modulation of AlO Dopamine Neurons by �y-Aminobutyric Peter W. Kalivas. Patricia Duffy and 858Acid Agonists Henry Eberhardt

Dopamine Efflux from Striatal Slices after Intracerebral 6- Gretchen L. Snyder. 867

Hydroxydopamine: Evidence for Compensatory Hyperactivity Richard W. Keller, Jr. andof Residual Terminals Michael J. Zigmond

Comparison of in Vitro and in Vivo Models of Drug William M. Pardridge, 884Transcytosis through the Blood-Brain Barrier Domingo Triguero, Jing Yang and

Pasquale A. Cancilla

Neurochemical and Toxic Effects of 1-Methyl-4-Phenyl- Linda K. Friedman and 892

I,2,3,6-Tetrahydropyridine and I-Methyl-4-Phenylpyridine to Catherine MytilineouRat Serotonin Neurons in Dissociated Cell Cultures

PHARMACOLOGY OF SUBSTANCE ABUSE

Behavioral Effects of N-Methylamphetamine and N,N- J. M. Witkin, G. A. Ricaurte and 466Dimethylamphetamine in Rats and Squirrel Monkeys J. L. Katz

Pharmacologic Characterization of the Sensitization to the Jill U. Adams and Stephen G. Holtzman 483Rate-Decreasing Effects of Naltrexone Induced by AcuteOpioid Pretreatment in Rats

Regional Changes in Sympathetic Nerve Activity and Martin Delle, Sven-Erik Ricksten, Jan 646Baroreceptor Reflex Function and Arterial Plasma Levels of Haggendal. Kerstin Olsson, Jon 0.Catecholamines, Renin and Vasopressin during Naloxone- Skarphedinsson and Peter Thor#{233}nprecipitated Morphine Withdrawal in Rats

Benzodiazepine Agonist and Inverse Agonist Actions on Kan J. Buck and R. Adron Hams 706GABAA Receptor-Operated Chloride Channels. I. AcuteEffects of Ethanol

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Benzodiazepine Agonist and Inverse Agonist Actions on Kari J. Buck and R. Adron Hams 713

GABAA Receptor-Operated Chloride Channels. II. ChronicEffects of Ethanol

PULMONARY PHARMACOLOGY

Bradykinin-Induced Bronchoconstriction in Guinea Pig in Masakazu Ichinose, Maria G. Belvisi and 594Vivo: Role of Neural Mechanisms Peter J . Barnes

RENAL PHARMACOLOGY

Mechanism of Uricosuric Action of AA-193 in DBA/2N Mice Takashi Dan, Haruko Tanaka and 437Hiroshi Koga

Transport of the Organic Cation N’-Methylnicotinamide by Kamel Besseghir, Dolorr#{232}sMosig and 444the Rabbit Proximal Tubule. I. Accumulation in the Isolated Fran#{231}oiseRoch-RamelNonperfused Tubule

Transport of the Organic Cation N’-Methylnicotinamide by Kamel Besseghir, Jean-Yves Chatton 452

the Rabbit Proximal Tubule. II. Reabsorption and Secretion and Fran#{231}oise Roch-Ramelin the Isolated Perfused Tubule

Thromboxane Mediates the Renal Hemodynamic Effects of Jae Yoo, Detlef Schlondorff and 743

Platelet Activating Factor Joel Neugarten

Contrasting Effects of Dopexamine Hydrochloride on Alan Stuart Bass 798

Electrolyte Excretion in Canine Kidney

TOXICOLOGY

Menthofuran-Dependent and Independent Aspects of David Thomassen, John T. Slattery and 567Pulegone Hepatotoxicity: Roles of Glutathione Sidney D. Nelson

ERRATA

Pharmacological Characterization of a Neuronal Receptor for Douglas A. Craig and David E. Clarke5-Hydroxytryptamine in Guinea Pig Ileum with PropertiesSimilar to the 5-Hydroxytryptamine4 Receptor (J. Pharmacol.Exp. Ther. 252: 1378-1386)

Gentamicin and Verapamil Compete for a Common Transport Paul P. Sokol, Kelly R. Huiatt,Mechanism in Renal Brush Border Membrane Vesicles (J. Peter D. Holohan and Charles R. RossPharmacol. Exp. Ther. 251: 937-942)

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TheJournalof

VOLUME 253

JUNE 1990NUMBER 3

PHARMACOLOGYAND EXPERIMENTAL THERAPEUTICS

ANALGESICS

Contents

Hypoglycemia Induced by Intrathecal Opioids in Mice:

Stereospecificity, Drug Specificity and Effect of Fasting

Brainstem Sites Differentially Sensitive to fl-Endorphin andMorphine for Analgesia and Release of Met-Enkephalin inAnesthetized Rats

Delta but Not Mu Opioid Receptors in the Spinal Cord areInvolved in Antinociception Induced by �-Endorphin GivenIntracerebroventricularly in Mice

AUTONOMIC PHARMACOLOGY

Role of Calcium in Adrenergic Neurochemical Transmissionin the Aging Heart

BEHAVIORAL PHARMACOLOGY

Comparative Behavioral, Neurochemical and PharmacologicalActivities of Dihydropyridine Calcium Channel ActivatingDrugs

Pharmacological Characterization of Cannabinoids in theElevated-Plus Maze

N-Methyl-i>aspartate Antagonism and Phencyclidine-like

Activity: A Drug Discrimination Analysis

Unusual Behavioral Profile of Alprazolam in SquirrelMonkeys

Body Temperature Differentially Affects Ethanol Sensitivityin Both Inbred Strains and Selected Lines of Mice

CARDIOVASCULAR PHARMACOLOGY

Interaction of Verapamil and Cimetidine: StereochemicalAspects of Drug Metabolism, Drug Disposition and DrugAction

Vascular Contraction Induced by Activation of MembraneCalcium Ion Channels is Enhanced in Streptozotocin-Diabetes

Electrophysiologic Effects of E-403i, a Class IIIAntiarrhythmic Agent, on Re-entrant VentricularArrhythmias in a Canine 7-day-old Myocardial InfarctionModel

in the Skin Microcirculation

Effects of the Potassium Channel Activator, BRL 34915, onthe Action Potential Characteristics of Canine CardiacPurkinje Fibers

Effect of Thromboxane Receptor Blockade on OxygenSupply/Consumption Variables during Reperfusion in theAnesthetized Dog

Deferoxamine Pretreatment Reduces Canine Infarct Size andOxidative Injury

State Dependence of Ethacizin and Ethmozin Block of SodiumCurrent in Voltage-Clamped and Internally Perfused CardiacPurkinje Cells

David A. Brase, Amrita K. Singha, 899

Uriel Estrada, Fred Lux and

William L. Dewey

Leon F. Tseng, Rui Tang, 930Robert Stackman, Amadou Camara andJames M. Fujimoto

Harold Hongwon Suh and 981

Leon Fu Tseng

Jay Roberts, Mary L. Mortimer, 957Patrick J. Ryan, Mark D. Johnson andNihal Turner

S. K. O’Neill, D. W. McKay, 905N. Campbell, C. R. Tnggle, M. Crowleyand 0. T. Bolger

Emmanuel S. Onaivi, Maude R. Green 1002and Billy R. Martin

Wouter Koek, James H. Woods and 1017

Francis C. Colpaert

Joseph 0. Wettstein 1070

D. A. Finn, M. Bejanian, B. J. Jones, 1229R. F. McGivern, P. J. Syapin,J. C. Crabbe and R. L. Alkana

Gerd Mikus, Michel Eichelbaurn, 1042Christine Fischer, Stanislaw Gumulka,Ulrich Klotz and Heyo K. Kroemer

Richard E. White and Gerald 0. Carrier 1057

Hiroshi Katoh, Satoshi Ogawa, 1077Izumi Furuno, Yoshihiro Sato,Shisei Yoh, Kimiko Saeki andYoshiro Nakarnura

Igor Stojanov and Kenneth G. Proctor 1083

Antoine Bril and Ricky Y. K. Man 1090

Gary J. Grover, PaulO. Sleph and 1097Harvey R. Weiss

Edward J. Lesnefsky, John E. Repine 1103and Lawrence D. Horwitz

Jonathan C. Makielski,Vladislav V. Nesterenko,William L. Nelson, A. I. Undrovinas,C. Frank Starmer andLeonid V. Rosenshtraukh

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Analysis of Cardiovascular and Pulmonary Responses to R. K. Minkes, J. A. Bellan, 1118Endothelin-1 and Endothelin-3 in the Anesthetized Cat R. M. Saroyan, M. D. Kerstein,

D. H. Coy, W. A. Murphy,B. D. Nossaman, D. B. McNamara andP. J. Kadowitz

Characterization of 5-Hydroxytryptamine Receptors on Lubo Zhang and Donald C. Dyer 1236Isolated Ovine Uterine Artery in Late Pregnancy

CELLULAR AND MOLECULAR PHARMACOLOGY

Stimulation of a Dopamine D1 Receptor Enhances Inositol Ashiwel S Undie and Eitan Friedman 987Phosphates Formation in Rat Brain

Two Dissociable Phases in the Contractile Response of the J. S. Fedan and S. J. Lamport 993Guinea Pig Isolated Vas Deferens to Adenosine Triphosphate

Thermodynamic Analyses of the Binding of Substrates and Jean-Jacques Bonnet, 1206

Uptake Inhibitors on the Neuronal Carrier of Dopamine Saloua Benmansour, Jean Costentin,

Labeled with I3HJGBR 12783 or f3HjMazindol Eric M. Parker and Luigi X. Cubeddu

Angiotensin II Desensitization and Ca�� and Na� Fluxes in Suma I. Shimuta, Celia A. Kanashiro, 1215Cultured Intestinal Smooth Muscle Cells Maria E. M. Oshiro, Therezinha B. Paiva

and Antonio C. M. Paiva

Effects of Histamine-Trifluoromethyl-Toluidide Derivative on Rong Qiu, Kenneth L. Melmon and 1245

Intracellular Calcium in Human Lymphocytes Manzoor M. Khan

Biochemical and Radiohistochemical Analyses of Alpha-2 Lan S. Chen, Jon B. Weingart and 1272

Adrenergic Receptors in the Kindling Model of Epilepsy James 0. McNamara

DEVELOPMENTAL PHARMACOLOGY

Pharmacokinetics and Dynamics of Furosemide in the Jeffrey J. Miceli, Paul A. Kramer, 1 126

Newborn Piglet Dennis J. Chapron, Ted S. Rosenkrantzand John R. Raye

DRUG METABOLISM AND DISPOSITION

Sequential Metabolism of Salicylamide Exclusively to Xin Xu, Bing K. Tang and 965

Gentisamide 5-Glucuronide and Not Gentisamide Sulfate K. Sandy PangConjugates in Single-Pass in Situ Perfused Rat Liver

ENDOCRINE PHARMACOLOGY

Inhibition of Endopeptidase 24.15 Greatly Increases the Abraham Lasdun and Marian Orlowski 1265Release of Luteinizing Hormone and Follicle Stimulating

Hormone in Response to Luteinizing Hormone/ReleasingHormone

GASTROINTESTINAL PHARMACOLOGY

Gastric Antiulcer and Cytoprotective Effects of Mohammad Tariq and 944Dipyridamole in Rats Abdulrehman M. Ageel

Inhibition of Bile Acid Transport by Cyclosporine A in Rat Richard H. Moseley, 974Liver Plasma Membrane Vesicles Timothy R. Johnson and

Jeffery M. Morrissette

Kappa Agonists Inhibit Gastric Emptying but Not Acid P. Lynn Touzeau and T. Shea-Donohue 1010

Secretion in Rhesus Monkeys

Effects of Zacopride and BMY25SOI (Batanopride) on Gregory L. King and 1026Radiation-Induced Emesis and Locomotor Behavior in the Michael R. LandauerFerret

Emesis and Defecations Induced by the 5-Hydroxytryptamine Gregory L. King 1034(5-HT3) Receptor Antagonist Zacopride in the Ferret

Regulation of the Neurotensin Receptor and Intracellular John T. Turner, Marilyn R. James- 1049Calcium Mobilization in HT29 Cells Kracke and Jean M. Camden

Effect of Endothelium-Derived Relaxing Factor on the Gastric Hisato Kitagawa, Fumiyo Takeda and 1133

Lesion Induced by HO in Rats Hiroshi Kohei

NEUROPHARMACOLOGY

Desensitization of Muscarinic Stimulated Hippocampal Cell Norbert J. Pontzer and Fulton T. Crews 921Firing is Related to Phosphoinositide Hydrolysis andInhibited by Lithium

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Contents continued on vi

Effects of Cocaine on Extrapyramidal and Limbic DynorphinSystems

Role of Opiates in Striatal D-1 Dopamine Receptor

Supersensitivity Induced by Chronic L-DOPA Treatment

Alpha-2 Adrenergic Inhibition of Ca�-Evoked 13H1Norepinephrine Release from Synaptosomes is Blocked byDepolarization

Ethanol Inhibits N-Methyl-r-Aspartate-Stimulated f3HJNorepinephrine Release from Rat Cortical Slices

Effects of Central Alpha-2 Adrenergic Compounds on Canine

Narcolepsy, a Disorder of Rapid Eye Movement Sleep

Kinetic and Dynamic Components of IncreasedBenzodiazepine Sensitivity in Aging Animals

5-HT2 Receptor Blockade by 10 169,369 and other 5-HT2Antagonists Modulates the Effects of D-2 Dopamine ReceptorBlockade

One Year of Continuous Treatment with Haloperidol orOozapine Fails to Induce a Hypersensitive Response ofCaudate Putamen Neurons to Dopamine Dl and D2 ReceptorAgonists

Effects of Acute and Chronic Administration of (+)-SKF10,047 on Body Temperature in the Rat: Cross-Sensitizationwith Phencyclidine

Pharmacological Evidence For Feedback Regulation ofDopamine Metabolism in Solid Fetal Substantia NigraTransplants

Chemically Induced Hypoglycemia and Anoxia: Relationshipto Glutamate Receptor-Mediated Toxicity in Retina

Acute- and Long-Term Glutamate-Mediated Regulation of

ICa�i in Rat Hippocampal Pyramidal Neurons in Vitro

PROSTAGLANDINS AND LEUKOTRIENES

Bacterial Sepsis-Induced Decrease in Lung VascularReactivity to 9,1 l-Dideoxy-1 la,9a-Epoxymethano-Prostaglandin F20 (U46619) in the Rat

PULMONARY PHARMACOLOGY

AHR-l43iOC: A Potent, Long-Acting, Nonsedating H1-Antihistamine that Prevents Antigen-Induced MucusFormation in Sensitive Rats

RENAL PHARMACOLOGY

Reserpine Up-Regulation of Rat Renal Cortical BetaAdrenergic Receptors is Independent of Its Effect on theSympathetic Nervous System

Furosemide Acts on Short Loop of Descending Thin Limb,but Not on Long Loop

Bumetanide-Induced Natriuresis and Antinatriuresis in theProximal and Distal Parts of the Human Nephron.Investigations in Acute and Chronic Bumetanide Treatment

TOXICOLOGY

Altered Synaptosomal Phospholipid Metabolism afterToluene: Possible Relationship with Membrane Fluidity,Na�,K�-Adenosine Triphosphatase and PhospholipidMethylation

Vitamin A Protects the Small Intestine from Methotrexate-Induce Damage in Rats

Patricia L. Smiley, Michel Johnson, 938Lloyd Bush, James W. Gibb andGlen R. Hanson

Antonio Groppetti, Gianpiera Ceresoli, 950

Virginio Mandelli and Marco Parenti

John F. Bowyer and Norman Weiner 1063

Rueben A. Gonzales and 1138John J. Woodward

Seiji Nishino, Laurel Haak,Heather Shepherd,Christian Guilleminault, Toshiaki Sakai,William C. Dement andEmmanuel Mignot

Jamie G. Barnhill, David J. Greenblatt, 1 153Lawrence 0. Miller, Anat Gayer,Jerold S. Harmatz and Richard I. Shader

Charles F. Saller, Michael J. Czupryna 1 162

and Andre I. Salama

Lian Hal Jiang, Richard J. Kasser, 1198C. Anthony Altar and Rex Y. Wang

M. Bejanian, R. N. Pechnick and 1253R. George

Rolando Meloni and Karen Gale 1259

Gail D. Zeevalk and William J. Nicklas 1285

Steven R. Glaum, Wendy K. Scholz and 1293Richard J. Miller

M. J. Schneidkraut and R. W. Carlson 1171

J. C. Nolan, M. H. Foxwell, 1177L. L. Whitman, J. M. Yanni,D. A. Walsh, B. F. Kilpatrick,D. N. Johnson and A. 0. Proakis

Timothy L. Fortin and 913

Pavur R. Sundaresan

Kyu Yong Jung and Hitoshi Endou 1184

Niels-Henrik Staalsen and Eva Steiness 1222

Carl P. LeBel and Robert A. Schatz 1189

Kazuyuki Tsurui, Yoshinori Kosakai, 1278Toshiharu Hone and Shoji Awazu

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TOXICOLOGY

Altered Synaptosomal Phospholipid Metabolism after Carl P. LeBel and Robert A. Schatz 1189Toluene: Possible Relationship with Membrane Fluidity,Na�,K�-Adenosine Triphosphatase and PhospholipidMethylation

Vitamin A Protects the Small Intestine from Methotrexate- Kazuyuki Tsurui, Yoshinori Kosakai, 1278Induce Damage in Rats Toshiharu Hone and Shoji Awazu

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