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

The kinetics of phenacetin O-deethylation and its inhibition by fluvox amine 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 flu voxamine-mediated inhibition of the reaction ranged from 2.7 to 14.5 n M, i.e. comparable to values obtained in human liver microsomes. The k inetic performance of the V79MZh1A2 cell line demonstrates its usefuln ess as an analytical tool in a variety of toxicological and drug metab olism studies involving CYP1A2.