[Biotransformation of amphetamine derivatives by rat liver mitochondria / 1st communication: Oxidative dealkylation of N,N-dialkyl- and N-alkylamphetamines (author's transl)].
Highly purified rat liver mitochondria catalyze oxidative dealkylation of N,N-dimethylamphetamine (I) and Methamphetamine (II). The demethylase activity is bound to the mitochondrial inner membrane or its matrix. Demethylation of N,N-dimethylaniline (1.231 nmol/mg/min) follows about two times faster than dealkylation of I (0.929 nmol/mg/min) or II (0.878 nmol/mg/min). Nitrazepam and other N-alkylamides seem to be no substrates for this mitochondrial enzyme at all. Under aerobic incubation conditions the rate of mitochondiral I-metabolism was about 1/8 of the microsomal rate, provided that both preparations have the some protein concentrations. NADPH was a much better cofactor for this reaction than NADH. The role of cytochrome P-450 as a possible essential cofactor for mitochondrial dealkylation could not be elucidated.
D000662:Amphetamines / Q000378:metabolism*; D001711:Biotransformation; D003640:Dealkylation; D008694:Methamphetamine / Q000031:analogs & derivatives / Q000378:metabolism; D008930:Mitochondria, Liver / Q000201:enzymology*; D009249:NADP / Q000378:metabolism; D010089:Oxidoreductases, N-Demethylating / Q000378:metabolism
D000662:Amphetamines; D008694:Methamphetamine; D009249:NADP; D010089:Oxidoreductases, N-Demethylating; C003714:dimethylamphetamine
Biotransformation von Amphetamin-Derivaten durch Rattenleber-Mitochondrien. 1. Mitt.: Oxidative Entalkylierung von N,N-Dialkyl- und N-Alkylamphetaminen.