羟基化
CYP3A4型
细胞色素P450
药物代谢
新陈代谢
酶
化学
CYP2D6型
体外
生物化学
CYP2C9
生物转化
微粒体
异源表达
代谢物
重组DNA
基因
作者
Qiang Li,Haihua Huang,Yu Dong,Dafang Zhong
出处
期刊:PubMed
日期:2005-10-01
卷期号:40 (10): 912-5
被引量:2
摘要
To identify the drug-metabolizing enzymes involved in the hydroxylation of the new anti-inflammatory and anodyne imrecoxib.Imrecoxib was incubated with heterologous expression human cytochrome P450 (rCYPs) in vitro, and metabolites and remained parent drug were detected with liquid chromatography-multistage mass spectrometry. The contribution of 4 CYPs in the hydroxylation metabolism of imrecoxib was evaluated by total normalized rate (TNR) method.Imrecoxib is metabolized by CYP2C9, CYP2D6 and CYP3A4, with the rate of 62.5%, 21.1% and 16.4%, respectively.CYP2C9 is the major enzyme involved in imrecoxib hydroxylation metabolism.
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