A P2Y12 receptor antagonist with antiplatelet activity
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Ticlopidine is a thienopyridine P2Y12 receptor antagonist.1 It inhibits aggregation of human platelets induced by collagen, arachidonic acid , and ADP .2 It also inhibits ADP-induced aggregation of rat platelets and decreases thrombus weight in vivo in a rat model of arterio-venous shunt thrombosis when administered at a dose of 100 mg/kg.3 Ticlopidine (300 mg/kg) inhibits healing of acetic acid-induced gastric ulcers in rats.4 Formulations containing ticlopidine have been used in the prevention of thrombotic stroke.
1.Porto, I., Giubilato, S., De Maria, G.L., et al.Platelet P2Y12 receptor inhibition by thienopyridines: Status and futureExpert Opin. Investig. Drugs18(9)1317-1332(2009) 2.Bruno, J.J.The mechanisms of action of ticlopidineThromb. Res. Suppl.459-67(1983) 3.Sugidachi, A., Asai, F., Ogawa, T., et al.The in vivo pharmacological profile of CS-747, a novel antiplatelet agent with platelet ADP receptor antagonist propertiesBr. J. Pharmacol.129(7)1439-1446(2000) 4.Ma, L., Elliott, S.N., Cirino, G., et al.Platelets modulate gastric ulcer healing: Role of endostatin and vascular endothelial growth factor releaseProc. Natl. Acad. Sci. USA98(11)6470-6475(2001)
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