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The P2Y₁₂ purinoceptor is a G protein-coupled ADP receptor found on platelets, mediating ADP-induced platelet activation and aggregation—a central component of hemostasis and thrombosis. Ticagrelor is an orally active, reversible antagonist of the P2Y₁₂ receptor; its major active metabolite AR-C124910XX shares this action. These agents block ADP-induced signal transduction, thereby preventing platelet activation and reducing risk of arterial thrombotic events, including myocardial infarction and stroke. In contrast to the thienopyridine class, ticagrelor and AR-C124910XX bind reversibly and do not require metabolic activation for efficacy.
Reversible, non-competitive antagonism of the P2Y₁₂ receptor, preventing ADP-mediated platelet activation and aggregation (for ticagrelor and its active metabolite); Irreversible antagonism of P2Y₁₂ receptor (for thienopyridines: clopidogrel, prasugrel, ticlopidine).
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