【摘 要】
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Clopidogrel is a prodrug which requires the metabolic activation by cytochrome P450 to generate its active metabolite.The active metabolite of clopidogrel c
【机 构】
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Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Dalian 116023
【出 处】
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2015年第一届药代动力学朝阳论坛
论文部分内容阅读
Clopidogrel is a prodrug which requires the metabolic activation by cytochrome P450 to generate its active metabolite.The active metabolite of clopidogrel can decrease the platelet activation and aggregation processes by inhibition the platelet P2Y12 andenosine diphosphate receptor.The generation of the active metabolite of clopidogrel via a two-steps catalytic reaction which involved multi-enzymes including CYP1A2, 2C19, 2B6, 2C9, 3A4, 3A5, 2B6, and serum paraoxonase 1.However, only 15% of clopidogrel is biotransformed into its active metabolite, around 85% clopidogrel is catalyzed by carboxylesterase 1 and generated an inactive metabolite clopidogrel carboxylic acid in vivo.
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