[Metabolic activation of N-methyl-N-nitrosourea in normal and tumor cells].
N-methyl-N-nitrosourea is metabolised by mouse liver microsomes yielding highly reactive product(s) capable of alkylating cellular macromolecules. Based on cofactor requirement (NADPH, oxygen), inhibition (NaN3) and induction by phenobarbital, 3,4-benz(a)pyrene, and MNU, the reaction is cytochrome P-450-dependent. Analysis of the kinetics and dose dependence of alkylation in vivo and in tissue homogenates confirms the fact that MNU must undergo metabolic activation in vivo.
D000477:Alkylating Agents; D000818:Animals; D001386:Azides / Q000494:pharmacology; D001580:Benzopyrenes / Q000494:pharmacology; D001711:Biotransformation; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism; D004790:Enzyme Induction; D008297:Male; D008770:Methylnitrosourea / Q000378:metabolism* / Q000494:pharmacology; D051379:Mice; D008862:Microsomes, Liver / Q000378:metabolism*; D009249:NADP / Q000494:pharmacology; D009607:Nitrosourea Compounds / Q000378:metabolism*; D010634:Phenobarbital / Q000494:pharmacology
D000477:Alkylating Agents; D001386:Azides; D001580:Benzopyrenes; D009607:Nitrosourea Compounds; D009249:NADP; D008770:Methylnitrosourea; D003577:Cytochrome P-450 Enzyme System; D010634:Phenobarbital
Metabolicheskaia aktivatsiia N-metil-N-nitrozomocheviny v normal'nykh i opukholevykh kletkakh.