Uridine 5'-diphosphate sodium salt is a selective native agonist of the P2Y6 receptor (EC50: 300 nM; pEC50: 6.52) and a potent antagonist of P2Y14 (pEC50: 7.28).
MRS2698 is an effective and highly selective agonist of the P2Y2 receptor (EC50: 8 nM). MRS2698 also is >300-fold P2Y2-selective versus the P2Y4 and P2Y6 receptors.
MRS2179 is a competitive P2Y1 receptor antagonist (Kb = 100 nM) with no appreciable activity at P2Y2, P2Y4, or P2Y6 at concentrations up to 30 µM, or at P2Y12 and P2Y13. It inhibits ADP-induced platelet shape change and aggregation (pA2 = 6.55) in vitro a
Potent and selective P2Y14 receptor agonist (EC50 = 0.92 nM). Exhibits >2000-fold selectivity over P2Y6. Das et al (2010) Human P2Y14 receptor agonists: truncation of the hexose moiety of uridine-5'-diphosphoglucose and its replacement with alkyl and aryl groups J.Med.Chem. 53 471 PMID:19902968 |Lazarowski et al (2015) UDP-sugars as extracellular signaling molecules: cellular and physiologic consequences of P2Y14 receptor activation. Mol.Pharmacol. 88 151 PMID:25829059