MRS2279 diammonium is a selective and high affinity P2Y1 receptor antagonist, with a K_i value of 2.5 nM and an IC₅₀ value of 51.6 nM. MRS2279 diammonium competitively inhibits ADP-promoted platelet aggregation with an pK_b value of 8.05.

MRS2279 diammonium antagonizes 2-MeSADP-stimulated inositol phosphate formation in turkey erythrocyte membranes with a pK_b value of 7.75.
MRS2279 diammonium shows high affinity competitive antagonism to human P2Y1 receptor with a pK_b value of 8.10 in 1321N1 human astrocytoma cells.
MRS2279 diammonium 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.
MRS2279 diammonium 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

MRS2279 diammonium (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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

MRS2279 diammonium (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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . 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.  [Content Brief]

  . Boyer JL, et al, Ravi RG, Jacobson KA, Harden TK. 2-Chloro N(6)-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate is a selective high affinity P2Y(1) receptor antagonist. Br J Pharmacol. 2002;135(8):2004-2010.  [Content Brief]

  . Wei W, et al. Mechanical ventilation induces lung and brain injury through ATP production, P2Y1 receptor activation and dopamine release. Bioengineered. 2022 Feb;13(2):2346-2359.  [Content Brief]