MRS2279

MRS2279 is a selective and high affinity P2Y1 receptor antagonist, with a K_i of 2.5 nM and an IC₅₀ of 51.6 nM. MRS2279 competitively inhibits ADP-promoted platelet aggregation with an apparent affnity (pK_B=8.05)^[1][2][3]. In Vitro:MRS2279 antagonizes 2-MeSADP-stimulated inositol phosphate formation in turkey erythrocyte membranes with a pK_b value of 7.75^[2].
MRS2279 shows high affinity competitive antagonism to human P2Y1 receptor with a pK_b value of 8.10 in 1321N1 human astrocytoma cells^[2].
MRS2279 shows specific effect for the P2Y1 receptor, but shows no effect on activation of the human P2Y2, P2Y4, P2Y6, or P2Y11 receptors by their cognate agonists^[2].
MRS2279 shows no ability to block the capacity of ADP to act through the Gi/adenylyl cyclase linked P2Y receptor of platelets to inhibit cyclic AMP accumulation^[2]. In Vivo:MRS2279 (2 μL, 1 nM; intracerebroventricular injection; 30 min prior to mechanical ventilation) reduces mouse brain injury induced by mechanical ventilation in high-pressure ventilation mice^[3].