MRS2179 tetrasodium hydrate

MRS2179tetrasodiumhydrate是一种竞争性P2Y1受体拮抗剂，对火鸡P2Y1受体的Kb值为102nM，pA2为6.99。MRS2179tetrasodiumhydrate对P2Y1的选择性高于P2X1(IC50=1.15&#181M)、P2X3(12.9&#181M)、P2X2、P2X4、P2Y2、P2Y4和P2Y6受体。MRS2179tetrasodiumhydrate抑制血小板聚集。

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Background

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.