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

Ming Liu, Yang Yan, Kan Gao, Yantong Sun, Du Xj, Tingting Yan, Jingkai Gu

Abstract

Objective To study the effect of O-desmethylvenlafaxine(ODV)on the content of cytochrome P450(CYP450)and activity of CYP2D6 and CYP3A4 in cytomicrosome of rat liver.Methods Rats 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(P0.05),while CYP2D6 activity was significantly reduced(P0.01)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.

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Key concepts: CYP3A4, CYP2D6, Microsome, Cytochrome P450, Enzyme, Pharmacology, Significant difference, Chemistry