KINETICS AND INHIBITION BY FLUVOXAMINE OF PHENACETIN O-DEETHYLATION IN V79 CELLS EXPRESSING HUMAN CYP1A2

被引：18

作者：

JENSEN, KG

POULSEN, HE

DOEHMER, J

LOFT, S

机构：

[1] UNIV COPENHAGEN,PANUM INST,DEPT PHARMACOL,DK-2200 COPENHAGEN,DENMARK

[2] TECH UNIV MUNICH,INST TOXICOL & ENVIRONM HYG,W-8000 MUNICH,GERMANY

来源：

PHARMACOLOGY & TOXICOLOGY | 1995年 / 76卷 / 04期

关键词：

D O I：

10.1111/j.1600-0773.1995.tb00144.x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The kinetics of phenacetin O-deethylation and its inhibition by fluvoxamine was investigated in a V79 cell line (V79MZh1A2) transfected with human CYP1A2. In four sets of experiments the apparent Km values for phenacetin O-deethylation ranged from 35 to 95 mu M and the Ki for fluvoxamine-mediated inhibition of the reaction ranged from 2.7 to 14.5 nM, i.e. comparable to values obtained in human liver microsomes. The kinetic performance of the V79MZh1A2 cell line demonstrates its usefulness as an analytical tool in a variety of toxicological and drug metabolism studies involving CYP1A2.

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收藏

页码：286 / 288

页数：3

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