The metabolism of 4-substituted-N-ethyl-N-methyl-anilines. II. Some factors influencing alpha-C- and N-oxidation.
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.
D000814:Aniline Compounds / Q000378:metabolism*; D000818:Animals; D002244:Carbon; D006224:Cricetinae; D006168:Guinea Pigs; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D008647:Mesocricetus; D051379:Mice; D008861:Microsomes / Q000201:enzymology; D010084:Oxidation-Reduction; D010088:Oxidoreductases / Q000378:metabolism; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D013045:Species Specificity
D000814:Aniline Compounds; C010951:N-ethyl-N-methylaniline; D002244:Carbon; D010088:Oxidoreductases