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Ticagrelor is a reversible antagonist of the platelet purinergic P2Y12 receptor (Ki = 14 nM; IC50 = 1.8 μM), which is the main receptor responsible for ADP-induced platelet aggregation.1,2 It functions by directly changing the conformation of the P2Y12 receptor to inhibit ADP binding.3 Formulations containing ticagrelor have been used to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome.
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1. Identification of high-
2. Advances in antiplatelet therapy. Hematology Am. Soc. Hematol. Educ. Program 2011(1), 62-69 (2011).
3. P2Y12 inhibitors: Differences in properties and mechanisms of action and potential consequences for clinical use. Eur. Heart J. 30(16), 1964-1977 (2009).
P2Y12 antagonist ticagrelor inhibits the release of procoagulant extracellular vesicles from activated platelets. Cardiol. J. 26(6), 782-789 (2019).