Human P2RY2

Figure. Concentration-dependent activation of P2RY2 by UTP

Reporter cells were transfected with either the expression plasmid for human purinergic receptor P2Y2 (P2RY2) or the mock plasmid and treated with various concentrations of UTP. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 1.5 µM.

purinergic receptor P2Y2
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
à la carte, Human non-orphan GPCRs

P2Y receptors

P2Y 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 [6], and the P2Y12 receptor antagonists prasugrel, ticagrelor and cangrelor, all approved as antiplatelet drugs [7,8].


  1. Burnstock G, Verkhratsky A. Purinergic signalling and the nervous system. 2012;None:1-715.
  2. Erlinge D. P2Y receptors in health and disease. Adv Pharmacol 2011;61:417-39.
  3. 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.
  4. von Kügelgen I, Harden TK. Molecular pharmacology, physiology, and structure of the P2Y receptors. Adv Pharmacol 2011;61:373-415.
  5. 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.
  6. Lau OC, Samarawickrama C, Skalicky SE. P2Y2 receptor agonists for the treatment of dry eye disease: a review. Clin Ophthalmol 2014;8:327-34.
  7. Capodanno D, Ferreiro JL, Angiolillo DJ. Antiplatelet therapy: new pharmacological agents and changing paradigms. J Thromb Haemost 2013;11 Suppl 1:316-29.
  8. 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

Related Receptors

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