- pyrimidinergic receptor P2Y4
- Available assay modes
- Agonist, Inverse agonist, Antagonist, PAM, NAM
- à la carte, Human non-orphan GPCRs
P2Y receptorsP2Y receptors are activated by the endogenous ligands ATP, ADP, uridine triphosphate, uridine diphosphate and UDP-glucose. The relationship of many of the cloned receptors to endogenously expressed receptors is not yet established and so it might be appropriate to use wording such as 'uridine triphosphate-preferring (or ATP-, etc.) P2Y receptor' or 'P2Y1-like', etc., until further, as yet undefined, corroborative criteria can be applied [1,2,3,4,5]. Clinically used drugs acting on these receptors include the dinucleoside polyphosphate diquafosol, agonist of the P2Y2 receptor subtype, approved in Japan for the management of dry eye disease , and the P2Y12 receptor antagonists prasugrel, ticagrelor and cangrelor, all approved as antiplatelet drugs [7,8].
- Burnstock G, Verkhratsky A. Purinergic signalling and the nervous system. 2012;None:1-715.
- Erlinge D. P2Y receptors in health and disease. Adv Pharmacol 2011;61:417-39.
- Jacobson KA. Structure-based approaches to ligands for G-protein-coupled adenosine and P2Y receptors, from small molecules to nanoconjugates. J Med Chem 2013;56:3749-67.
- von Kügelgen I, Harden TK. Molecular pharmacology, physiology, and structure of the P2Y receptors. Adv Pharmacol 2011;61:373-415.
- Weisman GA, Woods LT, Erb L, et al. P2Y receptors in the mammalian nervous system: pharmacology, ligands and therapeutic potential. CNS Neurol Disord Drug Targets 2012;11:722-38.
- Lau OC, Samarawickrama C, Skalicky SE. P2Y2 receptor agonists for the treatment of dry eye disease: a review. Clin Ophthalmol 2014;8:327-34.
- Capodanno D, Ferreiro JL, Angiolillo DJ. Antiplatelet therapy: new pharmacological agents and changing paradigms. J Thromb Haemost 2013;11 Suppl 1:316-29.
- Price MJ. Cangrelor: Pharmacology, Clinical Data, and Role in Percutaneous Coronary Intervention. Interv Cardiol Clin 2017;6:39-47.
Excerpt from IUPHAR/BPS Guide to Pharmacology
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