436847-09-5

MRS2365 is a potent and selective P2Y1 receptor (EC50=0.4 nM) /[35S]GTPγS binding/β-arrestin 2 recruitment agonist with an EC50 of 0.4 nM. MRS2365 relieves mechanical allodynia and increases mechanical sensitivity. MRS2365 shows little agonist or antagonist activity at the P2Y12 or P2Y13 receptors[1][2][3][4].

Highly potent, selective P2Y 1 receptor agonist (EC 50 = 0.4 nM). Displays no activity at P2Y 12 receptors and only very low agonist activity at P2Y 13 receptors (at concentrations up to 1 μ M).

P2Y1 Receptor: 0.4 nM (EC₅₀)

[1] Mariya Chhatriwala, et al. Induction of novel agonist selectivity for the ADP-activated P2Y1 receptor versus the ADP-activated P2Y12 and P2Y13 receptors by conformational constraint of an ADP analog. J Pharmacol Exp Ther. 2004 Dec;311(3):1038-43. DOI:10.1124/jpet.104.068650
[2] D M Bourdon, et al. (N)-methanocarba-2MeSADP (MRS2365) is a subtype-specific agonist that induces rapid desensitization of the P2Y1 receptor of human platelets. J Thromb Haemost. 2006 Apr;4(4):861-8. DOI:10.1111/j.1538-7836.2006.01866.x
[3] Andó RD, et al. A comparative analysis of the activity of ligands acting at P2X and P2Y receptor subtypes in models of neuropathic, acute and inflammatory pain. Br J Pharmacol. 2010 Mar;159(5):1106-17. DOI:10.1111/j.1476-5381.2009.00596.x
[4] Gao ZG, et al. Distinct Signaling Patterns of Allosteric Antagonism at the P2Y1 Receptor. Mol Pharmacol. 2017 Nov;92(5):613-626. DOI:10.1124/mol.117.109660