THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein-coupled receptors.

Alexander SPH; Arthur Christopoulos; Anthony P. Davenport; Kelly E; Mathie AA; Peters JA; Veale EL; Armstrong JF; Faccenda E; Harding SD; Pawson AJ; Sharman JL; Southan C; Davies JA

doi:10.1111/bph.14748

THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein-coupled receptors.

Alexander SPH, Arthur Christopoulos, Anthony P. Davenport, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA

British journal of pharmacology · 2019 · doi:10.1111/bph.14748 · PMID:31710717 · PMC6844580

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The 2019/20 Concise Guide to Pharmacology presents nomenclature and pharmacological tool summaries for nearly 1800 human drug targets, including G protein-coupled receptors, without specific findings related to endometriosis or adenomyosis.

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⚙ AI-generated deep summary by qwen3.7-flash, 2026-08-20 · read from full text ⓘ

This resource provides a comprehensive classification and pharmacological overview of G protein-coupled receptors, detailing their structural architecture, evolutionary relationships, and ligand specificities across various families such as rhodopsin-like, secretin, and metabotropic glutamate receptors. The authors catalog approximately 800 human GPCRs, distinguishing between sensory functions like olfaction and non-sensory roles mediated by diverse ligands, while also identifying orphan receptors with potential disease links or proposed endogenous ligands. Although the text includes extensive lists of receptor subtypes and pseudogenes, it does not present original experimental data but rather serves as a curated reference for existing knowledge on these membrane proteins. The paper does not explicitly discuss endometriosis or adenomyosis; it was included in the corpus via a keyword match in the upstream search index.

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Abstract

The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial publications. The Concise Guide provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide represents approximately 400 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.14748. G protein-coupled receptors are one of the six major pharmacological targets into which the Guide is divided, with the others being: ion channels, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2019, and supersedes data presented in the 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.

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Section

Vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase‐activating peptide (PACAP) receptors ( nomenclature as agreed by the NC‐IUPHAR Subcommittee on Vasoactive Intestinal Peptide Receptors [ http://www.ncbi.nlm.nih.gov/pubmed/9647867?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/22289055?dopt=AbstractPlus ]) are activated by the endogenous peptides http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1152 ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:12693 , http://www.uniprot.org/uniprot/P01282 ), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2258 ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:241 , http://www.uniprot.org/uniprot/P18509 ), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2257 ), peptide histidine isoleucineamide ( http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4397 {Mouse, Rat}), peptide histidine methionineamide ( http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2274 )) and peptide histidine valine ( http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3706 )). VPAC 1 and VPAC 2 receptors display comparable affinity for the PACAP peptides, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2257 ) and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2258 ), and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1152 ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:12693 , http://www.uniprot.org/uniprot/P01282 ), whereas http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2257 ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:241 , http://www.uniprot.org/uniprot/P18509 ) and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2258 ) are >100 fold more potent than http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1152 ) as agonists of most isoforms of the PAC 1 receptor. However, one splice variant of the human PAC 1 receptor has been reported to respond to http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2258 ), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2257 ) and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1152 ) with comparable affinity [ http://www.ncbi.nlm.nih.gov/pubmed/10583729?dopt=AbstractPlus ]. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2272 [ http://www.ncbi.nlm.nih.gov/pubmed/11068102?dopt=AbstractPlus ] has been used as a selective VPAC 2 receptor antagonist in a number of physiological studies, but has been reported to have significant activity at VPAC 1 and PAC 1 receptors [ http://www.ncbi.nlm.nih.gov/pubmed/16930633?dopt=AbstractPlus ]. The selective PAC 1 receptor agonist http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2264 , was extracted from the salivary glands of sand flies ( Lutzomyia longipalpis ) and has no sequence homology to http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1152 ) or the PACAP peptides [ http://www.ncbi.nlm.nih.gov/pubmed/8995389?dopt=AbstractPlus ]. Two deletion variants of http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2264 , http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3305 [ http://www.ncbi.nlm.nih.gov/pubmed/9928019?dopt=AbstractPlus ] and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2265 [ http://www.ncbi.nlm.nih.gov/pubmed/10438479?dopt=AbstractPlus ] have been reported to be PAC 1 receptor antagonists, but these peptides have not been extensively characterised. Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=370 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=371 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=372 HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:242 , http://www.uniprot.org/uniprot/P41586 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:12694 , http://www.uniprot.org/uniprot/P32241 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:12695 , http://www.uniprot.org/uniprot/P41587 Potency order of endogenous ligands http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2257 ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:241 , http://www.uniprot.org/uniprot/P18509 ), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2258 ) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1152 ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:12693 , http://www.uniprot.org/uniprot/P01282 ) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1152 ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:12693 , http://www.uniprot.org/uniprot/P01282 ), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2257 ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:241 , http://www.uniprot.org/uniprot/P18509 ), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2258 ) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2270 ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:4265 , http://www.uniprot.org/uniprot/P01286 ), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2273 {Pig}, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3643 ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:10607 , http://www.uniprot.org/uniprot/P09683 ) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1152 ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:12693 , http://www.uniprot.org/uniprot/P01282 ), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2258 ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:241 , http://www.uniprot.org/uniprot/P18509 ), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2257 ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:241 , http://www.uniprot.org/uniprot/P18509 ) > http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2273 {Pig} ≫ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2270 ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:4265 , http://www.uniprot.org/uniprot/P01286 ), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3643 ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:10607 , http://www.uniprot.org/uniprot/P09683 ) Selective agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2264 [ http://www.ncbi.nlm.nih.gov/pubmed/16930633?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2264 ] [ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3842 [ http://www.ncbi.nlm.nih.gov/pubmed/11931347?dopt=AbstractPlus ], [ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2278 [ http://www.ncbi.nlm.nih.gov/pubmed/10801840?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2259 [ http://www.ncbi.nlm.nih.gov/pubmed/9145428?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/10570056?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/11931347?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2276 [ http://www.ncbi.nlm.nih.gov/pubmed/9152366?dopt=AbstractPlus ] Selective antagonists – http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2268 (pIC 50 8.7) [ http://www.ncbi.nlm.nih.gov/pubmed/9437716?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/10570056?dopt=AbstractPlus ] – Labelled ligands http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2261 (Agonist) [ http://www.ncbi.nlm.nih.gov/pubmed/11193823?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2277 ) (Agonist) [ http://www.ncbi.nlm.nih.gov/pubmed/10801840?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2261 (Agonist) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2277 ) (Agonist) [ http://www.ncbi.nlm.nih.gov/pubmed/10801840?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2261 (Agonist) Subtypes of PAC 1 receptors have been proposed based on tissue differences in the potencies of http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2257 ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:241 , http://www.uniprot.org/uniprot/P18509 ) and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2258 ); these might result from differences in G protein coupling and second messenger mechanisms [ http://www.ncbi.nlm.nih.gov/pubmed/8967982?dopt=AbstractPlus ], or from alternative splicing of PAC 1 receptor mRNA [ http://www.ncbi.nlm.nih.gov/pubmed/8396727?dopt=AbstractPlus ]. Harmar AJ et al. (1998) International Union of Pharmacology. XVIII. Nomenclature of receptors for vasoactive intestinal peptide and pituitary adenylate cyclase‐activating polypeptide. Pharmacol Rev 50: 265‐270[ https://www.ncbi.nlm.nih.gov/pubmed/9647867?dopt=AbstractPlus ] Harmar AJ et al. (2012) Pharmacology and functions of receptors for vasoactive intestinal peptide and pituitary adenylate cyclase‐activating polypeptide: IUPHAR review 1. Br. J. Pharmacol. 166: 4‐17[ https://www.ncbi.nlm.nih.gov/pubmed/22289055?dopt=AbstractPlus ] Reglodi D et al. (2012) Effects of pituitary adenylate cyclase activating polypeptide in the urinary system, with special emphasis on its protective effects in the kidney. Neuropeptides 46: 61‐70[ https://www.ncbi.nlm.nih.gov/pubmed/21621841?dopt=AbstractPlus ] Smith CB et al. (2012) Is PACAP the major neurotransmitter for stress transduction at the adrenomedullary synapse? J. Mol. Neurosci. 48: 403‐12[ https://www.ncbi.nlm.nih.gov/pubmed/22610912?dopt=AbstractPlus ]

Overview

Adenosine receptors ( nomenclature as agreed by the NC‐IUPHAR Subcommittee on Adenosine Receptors [ http://www.ncbi.nlm.nih.gov/pubmed/11734617?dopt=AbstractPlus ]) are activated by the endogenous ligand http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2844 (potentially http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4554 also at A 3 receptors). Crystal structures for the antagonist‐bound [ http://www.ncbi.nlm.nih.gov/pubmed/22220592?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/18832607?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/22798613?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/27312113?dopt=AbstractPlus ], agonist‐bound [ http://www.ncbi.nlm.nih.gov/pubmed/25762024?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/21593763?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/21393508?dopt=AbstractPlus ] and G protein‐bound A 2A adenosine receptors [ http://www.ncbi.nlm.nih.gov/pubmed/27462812?dopt=AbstractPlus ] have been described. The structures of an antagonist‐bound A1 receptor [ http://www.ncbi.nlm.nih.gov/pubmed/28235198?dopt=AbstractPlus ] and an adenosine‐bound A1 receptor‐G i complex [ http://www.ncbi.nlm.nih.gov/pubmed/29925945?dopt=AbstractPlus ] have been resolved by cryo‐electronmicroscopy. Another structure of an antagonist‐bound A1 receptor obtained with X‐ray crystallography has also been reported [ http://www.ncbi.nlm.nih.gov/pubmed/28712806?dopt=AbstractPlus ]. Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=18 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=19 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=20 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=21 HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:262 , http://www.uniprot.org/uniprot/P30542 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:263 , http://www.uniprot.org/uniprot/P29274 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:264 , http://www.uniprot.org/uniprot/P29275 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:268 , http://www.uniprot.org/uniprot/P0DMS8 Endogenous agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2844 [ http://www.ncbi.nlm.nih.gov/pubmed/14662005?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2844 [ http://www.ncbi.nlm.nih.gov/pubmed/14662005?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2844 [ http://www.ncbi.nlm.nih.gov/pubmed/14662005?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2844 [ http://www.ncbi.nlm.nih.gov/pubmed/14662005?dopt=AbstractPlus ] Agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=377 [ http://www.ncbi.nlm.nih.gov/pubmed/15476669?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/7798201?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9920910?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/8300561?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/14662005?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=377 [ http://www.ncbi.nlm.nih.gov/pubmed/15267242?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9179373?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/15476669?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/7775460?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9920286?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/14662005?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=377 [ http://www.ncbi.nlm.nih.gov/pubmed/11093773?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/15267242?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/11266650?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/10496952?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/15194002?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/16219300?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/14662005?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=377 [ http://www.ncbi.nlm.nih.gov/pubmed/15267242?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/15476669?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9364471?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/8234299?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/10779381?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/14662005?dopt=AbstractPlus ] Selective agonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=380 [ http://www.ncbi.nlm.nih.gov/pubmed/9827575?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/15740718?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/15476669?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/16444290?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/16518376?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/7798201?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9920910?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6560 )‐ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6560 [ http://www.ncbi.nlm.nih.gov/pubmed/19317449?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5590 [ http://www.ncbi.nlm.nih.gov/pubmed/12672250?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=374 [ http://www.ncbi.nlm.nih.gov/pubmed/16518376?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/16020631?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=10235 [ http://www.ncbi.nlm.nih.gov/pubmed/30605331?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3290 [ http://www.ncbi.nlm.nih.gov/pubmed/11406470?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=8420 [ http://www.ncbi.nlm.nih.gov/pubmed/22324512?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/21393508?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=9236 [ http://www.ncbi.nlm.nih.gov/pubmed/22220592?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=375 [ http://www.ncbi.nlm.nih.gov/pubmed/15267242?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9179373?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/15476669?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/16518376?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/7775460?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9459566?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9920286?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/16020631?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5596 [ http://www.ncbi.nlm.nih.gov/pubmed/16518376?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3289 [ http://www.ncbi.nlm.nih.gov/pubmed/17353435?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=422 [ http://www.ncbi.nlm.nih.gov/pubmed/11705449?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/8126704?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9459566?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/10779381?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=457 [ http://www.ncbi.nlm.nih.gov/pubmed/10731034?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9364471?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/7932588?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=8421 [ http://www.ncbi.nlm.nih.gov/pubmed/22559880?dopt=AbstractPlus ] Antagonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=384 (p K i 8.5) [ http://www.ncbi.nlm.nih.gov/pubmed/9933143?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=404 (p K d 7.5) [ http://www.ncbi.nlm.nih.gov/pubmed/19317449?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=384 (p K i 7.7–9.4) [ http://www.ncbi.nlm.nih.gov/pubmed/9179373?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/7775460?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9459566?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9933143?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=404 (p K i 8.4–9) [ http://www.ncbi.nlm.nih.gov/pubmed/9179373?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9179373?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=404 (p K i 6.9–8.8) [ http://www.ncbi.nlm.nih.gov/pubmed/11093773?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/11266650?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/10624567?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9459566?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/10496952?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/15194002?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=384 (p K i 6–8.1) [ http://www.ncbi.nlm.nih.gov/pubmed/19141710?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/10624567?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9459566?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9933143?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/15194002?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=384 (p K i 7–7.9) [ http://www.ncbi.nlm.nih.gov/pubmed/8863790?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9459566?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9933143?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/10779381?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=404 (p K i 7–7.4) [ http://www.ncbi.nlm.nih.gov/pubmed/9459566?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/8234299?dopt=AbstractPlus ] Selective antagonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3285 (p K i 9.9) [ http://www.ncbi.nlm.nih.gov/pubmed/14563788?dopt=AbstractPlus ] – Rat, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=386 (p K i 7.4–9.2) [ http://www.ncbi.nlm.nih.gov/pubmed/15740718?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/8032613?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/16020631?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9920910?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/16902942?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3281 (p K i 9) [ http://www.ncbi.nlm.nih.gov/pubmed/17558436?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=8419 (p K i 8.8) [ http://www.ncbi.nlm.nih.gov/pubmed/8632314?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=9530 (p K i 7.4) [ http://www.ncbi.nlm.nih.gov/pubmed/28235198?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3283 (p K i 8.4–10.3) [ http://www.ncbi.nlm.nih.gov/pubmed/20801028?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/11087559?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=405 (p K i 8.8–9.1) [ http://www.ncbi.nlm.nih.gov/pubmed/9933143?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6561 (p K i 9.4) [ http://www.ncbi.nlm.nih.gov/pubmed/19569717?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3284 (p K i 9.3) [ http://www.ncbi.nlm.nih.gov/pubmed/19569717?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=449 (p K i 8.8) [ http://www.ncbi.nlm.nih.gov/pubmed/11266650?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/10737749?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3286 (p K i 7.3) [ http://www.ncbi.nlm.nih.gov/pubmed/11906291?dopt=AbstractPlus ] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=448 (p K i 8.2–9.2) [ http://www.ncbi.nlm.nih.gov/pubmed/9364471?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/8863790?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/11226132?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/16553647?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3280 (p K i 8.4) [ http://www.ncbi.nlm.nih.gov/pubmed/10841801?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=474 (p K i 7.7) [ http://www.ncbi.nlm.nih.gov/pubmed/9703464?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=470 (p K i 7.5) [ http://www.ncbi.nlm.nih.gov/pubmed/9364471?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/8917655?dopt=AbstractPlus , 1273 ] Allosteric modulators http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=9445 (Positive) [ http://www.ncbi.nlm.nih.gov/pubmed/2174510?dopt=AbstractPlus ] – – http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=9446 (Positive) [ http://www.ncbi.nlm.nih.gov/pubmed/16722654?dopt=AbstractPlus ], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=9447 (Positive) [ http://www.ncbi.nlm.nih.gov/pubmed/19161279?dopt=AbstractPlus ] Labelled ligands [ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=379 (Agonist) [ http://www.ncbi.nlm.nih.gov/pubmed/9459566?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9920910?dopt=AbstractPlus ], [ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=406 (Antagonist) (p K d 8.4–9.2) [ http://www.ncbi.nlm.nih.gov/pubmed/9827575?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/11705449?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9933143?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9920910?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/8300561?dopt=AbstractPlus ] [ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=455 (Antagonist) (p K d 8.7–9.1) [ http://www.ncbi.nlm.nih.gov/pubmed/11164377?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/10927024?dopt=AbstractPlus ], [ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=424 (Agonist) [ http://www.ncbi.nlm.nih.gov/pubmed/2600819?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/2213023?dopt=AbstractPlus ] [ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=453 (Antagonist) (p K d 9.8) [ http://www.ncbi.nlm.nih.gov/pubmed/11266650?dopt=AbstractPlus ] [ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=436 (Agonist) [ http://www.ncbi.nlm.nih.gov/pubmed/9933143?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/10779381?dopt=AbstractPlus ] Adenosine inhibits many intracellular ATP‐utilising enzymes, including adenylyl cyclase (P‐site). A pseudogene exists for the A 2B adenosine receptor ( https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:265 ) with 79% identity to the A 2B adenosine receptor cDNA coding sequence, but which is unable to encode a functional receptor [ http://www.ncbi.nlm.nih.gov/pubmed/7558011?dopt=AbstractPlus ]. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=386 also exhibits antagonism at A 2B receptors (p K i ca. 7,[ http://www.ncbi.nlm.nih.gov/pubmed/8937736?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/9459566?dopt=AbstractPlus ]). Antagonists at A 3 receptors exhibit marked species differences, such that only http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=474 and http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=470 are selective at the rat A 3 receptor. In the absence of other adenosine receptors, [ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=406 and [ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=455 can also be used to label A 2B receptors (KD ca . 30 and 60 nM respectively). [ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=436 also binds to A 1 receptors [ http://www.ncbi.nlm.nih.gov/pubmed/9459566?dopt=AbstractPlus ]. [ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=424 is relatively selective for A 2A receptors, but may also bind to other sites in cerebral cortex [ http://www.ncbi.nlm.nih.gov/pubmed/8692280?dopt=AbstractPlus , http://www.ncbi.nlm.nih.gov/pubmed/7566470?dopt=AbstractPlus ]. [ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=425 binds to other non‐receptor elements, which also recognise adenosine [ http://www.ncbi.nlm.nih.gov/pubmed/8937447?dopt=AbstractPlus ]. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3279 has been described as a fluorescent antagonist for labelling A 1 adenosine receptors in living cells, although activity at other adenosine receptors was not examined [ http://www.ncbi.nlm.nih.gov/pubmed/15070776?dopt=AbstractPlus ]. Borea PA et al . (2015) The A 3 adenosine receptor: history and perspectives. Pharmacol Rev 67 : 74‐102 [ https://www.ncbi.nlm.nih.gov/pubmed/25387804?dopt=AbstractPlus ] Cronstein BN et al . (2017) Adenosine and adenosine receptors in the pathogenesis and treatment of rheumatic diseases. Nat Rev Rheumatol 13 : 41‐51 [ https://www.ncbi.nlm.nih.gov/pubmed/27829671?dopt=AbstractPlus ] Fredholm BB et al . (2011) International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors–an update. Pharmacol Rev 63 : 1‐34 [ https://www.ncbi.nlm.nih.gov/pubmed/21303899?dopt=AbstractPlus ] Guo D et al . (2017) Kinetic Aspects of the Interaction between Ligand and G Protein‐Coupled Receptor: The Case of the Adenosine Receptors. Chem Rev 117 : 38‐66 [ https://www.ncbi.nlm.nih.gov/pubmed/27088232?dopt=AbstractPlus ] Göblyös A et al . (2011) Allosteric modulation of adenosine receptors. Biochim Biophys Acta 1808 : 1309‐18 [ https://www.ncbi.nlm.nih.gov/pubmed/20599682?dopt=AbstractPlus ] Lasley RD. (2011) Adenosine receptors and membrane microdomains. Biochim Biophys Acta 1808 : 1284‐9 [ https://www.ncbi.nlm.nih.gov/pubmed/20888790?dopt=AbstractPlus ] Mundell S et al . (2011) Adenosine receptor desensitization and trafficking. Biochim Biophys Acta 1808 : 1319‐28 [ https://www.ncbi.nlm.nih.gov/pubmed/20550943?dopt=AbstractPlus ] Vecchio EA et al . (2018) New paradigms in adenosine receptor pharmacology: allostery, oligomerization and biased agonism. Br J Pharmacol 175 : 4036‐4046 [ https://www.ncbi.nlm.nih.gov/pubmed/29679502?dopt=AbstractPlus ] Wei CJ etal . (2011)Normaland abnormalfunctions ofadenosine receptors inthecentral nervous system revealed by genetic knockout studies. Biochim Biophys Acta 1808 : 1358‐79[ https://www.ncbi.nlm.nih.gov/pubmed/21185258?dopt=AbstractPlus ]

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