2-Methylthio-AMP diTEA

2-Methylthio-AMP (2-MeSAMP) diTEA is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP diTEA is an inhibitor of ADP-dependent platelet aggregation[1][2][3].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> P2Y Receptor

P2Y12[1]

2-Methylthio-AMP (2-MeSAMP) diTEA inhibits agonist-mediated αIIbβ3 activation in platelets[1]. 2-methylthio-AMP (50 μM; for 5 minutes) diTEA does not significantly inhibit thrombin, PAR1-AP, PAR4-AP, or ADP-mediated platelet Ca2+ mobilization. 2-methylthio-AMP diTEA fails to inhibit Ca2+ mobilization in P2Y12-deficient mouse platelets and does not raise cAMP or induce vasodilator-stimulated phosphoprotein phosphorylation in wild-type platelets[1].

[1]. John H Cleator, et al. Racial differences in resistance to P2Y12 receptor antagonists in type 2 diabetic subjects. J Pharmacol Exp Ther. 2014 Oct;351(1):33-43.

[2]. Bernhard H Rauch, et al. Regulation of functionally active P2Y12 ADP receptors by thrombin in human smooth muscle cells and the presence of P2Y12 in carotid artery lesions. Arterioscler Thromb Vasc Biol. 2010 Dec;30(12):2434-42.

[3]. A Malinin, et al. Validation of a VerifyNow-P2Y12 cartridge for monitoring platelet inhibition with clopidogrel. Methods Find Exp Clin Pharmacol. 2006 Jun;28(5):315-22.