The metabolism of 4-substituted-N-ethyl-N-methyl-anilines. II. Some factors influencing alpha-C- and N-oxidation

Abstract

A g.l.c. method for the quantification of N-demethylated and/or N-de-ethylated (alpha-C-oxidation) and N-oxidation products of several 4-substituted-N-ethyl-N-methylanilines is described. Factors affecting the metabolism of these tertiary anilines in vitro have been studied and conditions which allow maximal metabolism established. The alpha-C- and N-oxidase activity was detected principally in the liver, lung, kidney and bladder microsomal fraction. A species difference in the extent of metabolism was evident, the order of activity not being the same for alpha-C- as that for N-oxidation. The pKa but not log P values determined for the teritary anilines appear to influence the apparent Km for both alpha-C- and N-oxidation.