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药物代谢酶细胞色素P450 2C9研究进展
引用本文:陈騉,王睿. 药物代谢酶细胞色素P450 2C9研究进展[J]. 中国临床药理学与治疗学, 2004, 9(6): 601-606
作者姓名:陈騉  王睿
作者单位:1. 中国海洋大学,海洋药物与食品研究所药理室,青岛,266003,山东
2. 解放军总医院临床药理室,北京,100853
基金项目:国家 8 63计划支持项目 (№ :2 0 0 2AA2Z3 41L)
摘    要:P450 2C9是人体中重要的药物代谢酶。P450 2C9基因编码区的多态性造成氨基酸序列的变化。主要包括P450 2C9*2和P450 2C9*3两种突变体,变异纯合子对P450 2C9底物的代谢能力明显降低。P450 2C9的底物包括甲苯磺丁脲、苯妥英、S-法华令、氟西汀、洛沙坦等。P450 2C9可被利福平诱导,被胺碘酮和氟康唑等多种药物抑制。

关 键 词:细胞色素P450 2C9 基因多态性 药物代谢 遗传药理学
文章编号:1009-2501(2004)06-0601-06
修稿时间:2003-01-14

Advance of drug metabolism enzyme P450 2C9
CHEN Kun,WANG Rui. Advance of drug metabolism enzyme P450 2C9[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2004, 9(6): 601-606
Authors:CHEN Kun  WANG Rui
Affiliation:CHEN Kun,WANG Rui 1 Department of Pharmacology,Institute of Marine Drug and Food,Ocean University of China,Qingdao,266003,Shandong,China, 1 Department of Clinical Pharmacology,General Hospital of the Chinese People's Liberation Army,Beijing,100853,China
Abstract:P450 2C9 is the most important drug metabolizing enzymes in humans. Polymorphisms in P450 2C9 gene produce variants at amino acid including P450 2C9*2 and P450 2C9*3. Metabolic capacities for P450 2C9 substrates are diminished by individuals of homozygous. P450 2C9 substrates mainly include tolbutamide, phenytoin, S-warfarin, fluoxetine, and losartan. P450 2C9 can be induced by rifampin and inhibited by amiodarone and fluconazole.
Keywords:P450 2C9  genetic polymorphism  drug metabolism  pharmacogenetics
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