Structure reactivity relationships in the microsomal oxidation of tertiary amines

Apparent kinetic parameters Vmax and KM have been measured for the oxidative N-demethylation of twelve para-substituted N, N-dimethylanilines catalysed by rat liver microsomes. Vmax was enhanced by pretreatment of the rats with phenobarbital, whereas pretreatment with beta-naphthoflavone gave no appreciable enhancement. In the case of phenobarbital pretreatment the kinetic parameters could be expressed in terms of lipophilic and electronic effect of the substituents. Kinetic parameters from control and beta-naphthoflavone microsomes gave no statistically meaningful correlation.