Update of P2Y receptor pharmacology : IUPHAR Review 27
Jacobson, Kenneth A. and Delicado, Esmerilda G. and Gachet, Christian and Kennedy, Charles and von Kügelgen, Ivar and Li, Beibei and Miras-Portugal, M. Teresa and Novak, Ivana and Schöneberg, Torsten and Perez-Sen, Raquel and Thor, Doreen and Wu, Beili and Yang, Zhenlin and Müller, Christa E. (2020) Update of P2Y receptor pharmacology : IUPHAR Review 27. British Journal of Pharmacology, 177 (11). 2413–2433. ISSN 1476-5381
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Abstract
Eight G protein-coupled P2Y receptor subtypes respond to extracellular adenine and uracil mononucleotides and dinucleotides. P2Y receptors belong to the δ group of rhodopsin-like GPCRs and contain two structurally distinct subfamilies: P2Y 1, P2Y 2, P2Y 4, P2Y 6, and P2Y 11 (principally G q protein-coupled P2Y 1-like) and P2Y 12–14 (principally G i protein-coupled P2Y 12-like) receptors. Brain P2Y receptors occur in neurons, glial cells, and vasculature. Endothelial P2Y 1, P2Y 2, P2Y 4, and P2Y 6 receptors induce vasodilation, while smooth muscle P2Y 2, P2Y 4, and P2Y 6 receptor activation leads to vasoconstriction. Pancreatic P2Y 1 and P2Y 6 receptors stimulate while P2Y 13 receptors inhibits insulin secretion. Antagonists of P2Y 12 receptors, and potentially P2Y 1 receptors, are anti-thrombotic agents, and a P2Y 2/P2Y 4 receptor agonist treats dry eye syndrome in Asia. P2Y receptor agonists are generally pro-inflammatory, and antagonists may eventually treat inflammatory conditions. This article reviews recent developments in P2Y receptor pharmacology (using synthetic agonists and antagonists), structure and biophysical properties (using X-ray crystallography, mutagenesis and modelling), physiological and pathophysiological roles, and present and potentially future therapeutic targeting.
Creators(s): |
Jacobson, Kenneth A., Delicado, Esmerilda G., Gachet, Christian, Kennedy, Charles ![]() | Item type: | Article |
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ID code: | 72461 |
Keywords: | GPCR, G protein-coupled receptor, nucleotide receptors, P2Y receptors, nucleotides, Pharmacy and materia medica, Pharmacology, Toxicology and Pharmaceutics(all) |
Subjects: | Medicine > Pharmacy and materia medica |
Department: | Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences |
Depositing user: | Pure Administrator |
Date deposited: | 26 May 2020 10:23 |
Last modified: | 22 Jan 2021 04:01 |
URI: | https://strathprints.strath.ac.uk/id/eprint/72461 |
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