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

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Abstract
1. A g.l.c. method for the quantification of N-demethylated and/or N-de-ethylated (α-C-oxidation) and N-oxidation products of several 4-substituted-N-ethyl-N-methylanilines is described. 2. Factors affecting the metabolism of these tertiary anilines in vitro have been studied and conditions which allow maximal metabolism established. 3. The α-C- and N-oxidase activity was detected principally in the liver, lung, kidney and bladder microsomal fraction. 4. A species difference in the extent of metabolism was evident, the order of activity not being the same for α-C- as that for N-oxidation. 5. The pKa but not log P values determined for the tertiary anilines appear to influence the apparent Km for both α-C- and N-oxidation.