O-去甲基文拉法辛对大鼠肝微粒体细胞色素P450酶含量及CYP2D6、CYP3A4活性的影响  

Effect of O-desmethylvenlafaxine on the content of cytomicrosome cytochrome P450 (CYP450) enzyme and activity of CYP2D6 and CYP3A4 in rat liver

作　　者：刘明远[1] 杨艳[1] 高瞰[1] 孙严彤[1] 杜晓琳[1] 闫婷婷[1] 顾景凯[1] 

机构地区：[1]吉林大学药物代谢研究中心,吉林长春130021

出　　处：《中国老年学杂志》2007年第7期632-633,共2页Chinese Journal of Gerontology

摘　　要：目的研究O-去甲基文拉法辛对大鼠肝微粒体内细胞色素P450(CYP450)含量及CYP2D6、CYP3A4活性的影响。方法生理盐水为对照,大鼠灌胃22.90mg.kg-1.d-1的O-去甲基文拉法辛琥珀酸盐一水合物,连续7d,然后测定其肝微体中CYP450含量及CYP2D6、CYP3A4活性。结果与生理盐水组比较,ODV组CYP450含量和CYP3A4活性无变化(P>0.05),CYP2D6活性明显被抑制(P<0.01)。结论ODV对CYP450含量和CYP3A4活性无影响,但对CYP2D6活性有抑制作用。Objective To study the effect of O-desmethylverdafaxine （ODV） on the content of cytochrome P450 （CYP450） and activity of CYP2D6 and CYP3A4 in cytomicrosome of rat liver. Methods Bats were given 4.58 mg · kg^-1 · d^-1 ODV monohydrate for 7 days to detect the content of CYP450, activity of CYP2D6 and CYP3A4 in liver microsome taking normal sodium as control group. Results CYP450 content and CYP3A4 activity of liver microsome had no difference （P 〉0.05）, while CYF2D6 activity was significantly reduced （P 〈0.01 ）in ODV group compared with those in control group. Conclusions ODV shows no effect on CYP450 content and CYP3A4 activity, but can inhibit CYP2D6 activity in liver microsomes.

关 键 词：O-去甲基文拉法辛 CYP450 CYP2D6 CYP3A4 

分 类 号：R969.1[医药卫生—药理学]