MRS2179 is a competitive purinergic P2Y₁receptor antagonist (K_b= 102 nM).¹It is selective for P2Y₁over P2Y₂, P2Y₄, P2Y₆, P2Y₁₂, and P2Y₁₃, as well as P2X_1-4, receptors at 10 µM.^2,3MRS2179 reduces phospholipase C (PLC) activity induced by the P2Y receptor agonist 2-methylthioadenosine diphosphate with an IC₅₀value of 331 nM in turkey erythrocyte membranes that endogenously express high levels of the P2Y₁receptor.¹It inhibits platelet shape change and aggregation induced by ADP in washed isolated human platelets when used at a concentration of 10 µM.⁴MRS2179 (50 mg/kg, i.v.) prolongs the length of tail bleeding time in mice, as well as decreases platelet thrombus formation in a mouse model of iron chloride-induced arterial thrombosis.^4,5

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