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http://onlinelibrary.wiley.com/doi/10.1111/bph.12444/fullhttp://www.guidetopharmacology.org/index.jsphttp://onlinelibrary.wiley.com/doi/10.1111/bph.12445/abstracthttp://onlinelibrary.wiley.com/doi/10.1111/bph.12444/abstracthttp://www.guidetopharmacology.org/http://onlinelibrary.wiley.com/doi/10.1111/bph.12444/fullhttp://www.guidetopharmacology.org/mailto:[email protected]

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http://onlinelibrary.wiley.com/doi/10.1111/bph.12444/fullhttp://www.guidetopharmacology.org/index.jsphttp://onlinelibrary.wiley.com/doi/10.1111/bph.12450/abstracthttp://onlinelibrary.wiley.com/doi/10.1111/bph.12449/abstracthttp://onlinelibrary.wiley.com/doi/10.1111/bph.12448/abstracthttp://onlinelibrary.wiley.com/doi/10.1111/bph.12447/abstracthttp://onlinelibrary.wiley.com/doi/10.1111/bph.12446/abstract

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Conflict of interest

The authors state that there are no conflicts of interest to disclose.

List of records presented

1454 Adiponectin receptors1455 Fatty acid binding proteins1457 Sigma receptors

S.P.H. Alexanderet al. The Concise Guide to PHARMACOLOGY 2013/14: Overview. British Journal of Pharmacology (2013) 170, 14491458

Searchable database:http://www.guidetopharmacology.org/index.jsp Overview 1453

Full Contents of Concise Guide:http://onlinelibrary.wiley.com/doi/10.1111/bph.12444/full
http://www.guidetopharmacology.org/index.jsphttp://onlinelibrary.wiley.com/doi/10.1111/bph.12444/fullhttp://onlinelibrary.wiley.com/doi/10.1111/bph.12444/fullhttp://www.guidetopharmacology.org/index.jsp

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http://onlinelibrary.wiley.com/doi/10.1111/bph.12444/fullhttp://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=106http://www.guidetopharmacology.org/index.jsphttp://www.ncbi.nlm.nih.gov/pubmed/21718299?dopt=AbstractPlushttp://www.ncbi.nlm.nih.gov/pubmed/19207481?dopt=AbstractPlushttp://www.ncbi.nlm.nih.gov/pubmed/19359049?dopt=AbstractPlushttp://www.ncbi.nlm.nih.gov/pubmed/23017711?dopt=AbstractPlushttp://www.ncbi.nlm.nih.gov/pubmed/19029992?dopt=AbstractPlushttp://www.ncbi.nlm.nih.gov/pubmed/22547160?dopt=AbstractPlushttp://www.ncbi.nlm.nih.gov/pubmed/20875820?dopt=AbstractPlushttp://www.uniprot.org/uniprot/P55290http://www.genenames.org/data/hgnc_data.php?hgnc_id=1753http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3726http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3727http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3726http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3727http://www.uniprot.org/uniprot/Q86V24http://www.genenames.org/data/hgnc_data.php?hgnc_id=24041http://www.uniprot.org/uniprot/Q96A54http://www.genenames.org/data/hgnc_data.php?hgnc_id=24040http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=650http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=649http://www.uniprot.org/uniprot/Q9UKG1http://www.genenames.org/data/hgnc_data.php?hgnc_id=24035http://www.uniprot.org/uniprot/Q15848http://www.genenames.org/data/hgnc_data.php?hgnc_id=13633http://www.ensembl.org/Homo_sapiens/Gene/Family/Genes?family=ENSFM00500000270960http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=106

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Preferred abbreviation RBP7 RLBP1 CRABP1 CRABP2

Nomenclature retinol binding protein 7, cellular retinaldehyde binding protein 1 cellular retinoic acid binding protein 1 cellular retinoic acid binding protein 2

HGNC, UniProt RBP7, Q96R05 RLBP1, P12271 CRABP1,P29762 CRABP2, P29373

Rank order of potency 11-cis-retinal,11-cis-retinol > 9-cis-retinal,13-cis-retinal,13-cis-retinol,all-trans-retinal,retinol[8]

all-trans-retinoic acid > 9-cis-retinoic acidstearic acid >palmitic acid,oleic acid,linoleic acid, -linolenic acid,arachidonicacid[14]

Comments: Although not tested at all FABPs, BMS309403 exhibits high affinity for FABP4 (pIC50 8.8) compared to FABP3 or FABP5 (pIC50

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Sigma receptors

Overview: Although termed receptors, the evidence for coupling through conventional signalling pathways is lacking. Initially described as a subtype of opioid receptors, there is only a modestpharmacological overlap and no structural convergence with the G protein-coupled receptors. A wide range of compounds, ranging from psychoactive agents to antihistamines, have been observed tobind to these sites, which appear to be intracellular.

Nomenclature 1(sigma non-opioid intracellular receptor 1) 2

HGNC, UniProt SIGMAR1, Q99720

Selective agonists (+)-SK&F10047,(RS)-PPCC(pKi8.8)[25],PRE-084(pIC507.4)[26] PB-28(pKi8.3)[21]

Selective antagonists NE-100(pIC508.4)[24],BD-1047(pIC507.4)[23] (RS)-SM21(pIC507.2)[22]

Radioligands (Kd) [3H]-pentazocine(Agonist) [3H]-di-o-tolylguanidine(Agonist)

Comments: (-)-pentazocinealso shows activity at opioid receptors. There is no molecular correlate of the sigma2 receptor.

Further reading

de Medina P, Paillasse MR, Sgala G, Khallouki F, Brillouet S, Dalenc F, Courbon F, Record M, PoirotM, Silvente-Poirot S. (2011) Importance of cholesterol and oxysterols metabolism in thepharmacology of tamoxifen and other AEBS ligands. Chem Phys Lipids 164: 432437.[PMID:21641337]

Dubrovsky B. (2006) Neurosteroids, neuroactive steroids, and symptoms of affective disorders.Pharmacol Biochem Behav84: 644655. [PMID:16962651]

Guitart X, Codony X, Monroy X. (2004) Sigma receptors: biology and therapeutic potential.Psychopharmacology (Berl) 174: 301319. [PMID:15197533]

Matsumoto RR, Liu Y, Lerner M, Howard EW, Brackett DJ. (2003) Sigma receptors: potentialmedications development target for anti-cocaine agents. Eur J Pharmacol 469: 112.

[PMID:12782179]


Searchable database:http://www.guidetopharmacology.org/index.jsp Sigma receptors 1457

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