MRS2179 tetrasodium hydrate is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium hydrate is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors[1][2]. MRS2179 tetrasodium hydrate inhibits platelet aggregation[3].
MRS2179 tetrasodium hydrate (50 mg/kg; i.p.) prolongs the bleeding time[3]. Animal Model: CL57BLr6 mice[3]
[1]. Nandanan E, et al. Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y(1) receptor ligands. J Med Chem. 2000;43(5):829-842. [2]. von KÜgelgen I. Pharmacological profiles of cloned mammalian P2Y-receptor subtypes. Pharmacol Ther. 2006;110(3):415-432. [3]. Baurand A, Raboisson P, Freund M, et al. Inhibition of platelet function by administration of MRS2179, a P2Y1 receptor antagonist. Eur J Pharmacol. 2001;412(3):213-221.