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

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 pK_a but not log P values determined for the tertiary anilines appear to influence the apparent K_m for both α-C- and N-oxidation.