Hepatic microsomal enzyme induction by trifluoromethyl compounds and some halogenated and nonhalogenated analogs.
Trifluoromethyl derivatives of toluene, phenothiazine, benzimidazole and DDT were administered ip to male rats for 5 days and induction of hepatic microsomal enzymes catalyzing the metabolism of EPN, p-nitroanisole and aminopyrine measured. The addition of a trifluoromethyl substituent to toluene, phenothiazine and benzimidazole increased the inducing capacity of the parent molecule on p-nitroanisole metabolism. Dihalogenation of benzene with trifluoromethyl groups, regardless of position, resulted in induction of p-nitroanisole metabolism whereas halogenation of benzene with trichloromethyl groups did not. For these compounds, the size and electron-inducing capacity of the halogenated substituent may be relative to microsomal enzyme induction.
D000633:Aminopyrine N-Demethylase / Q000378:metabolism; D000818:Animals; D001562:Benzimidazoles / Q000494:pharmacology; D003634:DDT / Q000494:pharmacology; D004790:Enzyme Induction / Q000187:drug effects*; D006845:Hydrocarbons, Fluorinated / Q000494:pharmacology* / Q000633:toxicity; D007928:Lethal Dose 50; D008297:Male; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology*; D009575:Nitroanisole O-Demethylase / Q000378:metabolism; D010640:Phenothiazines / Q000494:pharmacology; D004849:Phenylphosphonothioic Acid, 2-Ethyl 2-(4-Nitrophenyl) Ester / Q000378:metabolism; D051381:Rats; D014268:Trifluoperazine / Q000494:pharmacology
D001562:Benzimidazoles; D006845:Hydrocarbons, Fluorinated; D010640:Phenothiazines; D004849:Phenylphosphonothioic Acid, 2-Ethyl 2-(4-Nitrophenyl) Ester; D014268:Trifluoperazine; D003634:DDT; D009575:Nitroanisole O-Demethylase; D000633:Aminopyrine N-Demethylase