Kinetics and Inhibition by Fluvoxamine of Phenacetin O‐Deethylation in V79 Cells Expressing Human CYP1A2
- 1 April 1995
- journal article
- Published by Wiley in Basic & Clinical Pharmacology & Toxicology
- Vol. 76 (4) , 286-288
- https://doi.org/10.1111/j.1600-0773.1995.tb00144.x
Abstract
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 microM 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.Keywords
This publication has 9 references indexed in Scilit:
- Selective serotonin reuptake inhibitors and theophylline metabolism in human liver microsomes: potent inhibition by fluvoxamine.British Journal of Clinical Pharmacology, 1995
- Effects of benzo[a]pyrene and (±)-trans-7,8-dihydroxy-7,8-dihydrobenzo[a]pyrene on mitosis in Chinese hamster V79 cells with stable expression of rat cytochrome P4501A1 or 1A2Carcinogenesis: Integrative Cancer Research, 1993
- Cytogenetic effects of promutagens in genetically engineered V79 chinese hamster cells expressing cytochromes P450European Journal of Pharmacology: Environmental Toxicology and Pharmacology, 1993
- Fluvoxamine is a potent inhibitor of cytochrome P4501A2Biochemical Pharmacology, 1993
- Metabolism of phenacetin in V79 Chinese hamster cell cultures expressing rat liver cytochrome P4501A2 compared to isolated rat hepatocytesBiochemical Pharmacology, 1993
- Genetically engineered V79 Chinese hamster cells for stable expression of human cytochrome P450IA2European Journal of Pharmacology: Environmental Toxicology and Pharmacology, 1992
- Biotransformation of caffeine and theophylline in mammalian cell lines genetically engineered for expression of single cytochrome P450 isoformsBiochemical Pharmacology, 1992
- Applications of stable V79-derived cell lines expressing rat cytochromes P4501A1, 1A2, and 2B1Xenobiotica, 1992
- The use of genetically engineered V79 Chinese hamster cultures expressing rat liver CYP1A1, 1A2 and 2B1 cDNAs in micronucleus assaysMutagenesis, 1991