Aminopyrine-N-demethylase. I. Directed modification of substrates' structure as a way of production of inducer of the monooxygenase isoform P-450b.
The effect of the phenobarbital-type monooxygenase inducers is accomplished via the native molecule. This made it possible to transform the typical substrate of cytochrome P-450b aminopyrine into an inducer of this isozyme by blocking the substrate molecule position undergoing monooxygenation. Substitution of two methyl groups in the aminopyrine -N(CH3)2 position by an isopropyl group gave rise to a clear-cut inducive effect. This was registered by spectral, kinetic, radiological and immunochemical methods.
Tsyrlov
I B
IB
Laboratory of Xenobiochemistry, Academy of Medical Sciences, Siberian Division, Novosibirsk, USSR.
Gerasimov
K E
KE
D000632:Aminopyrine / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D000633:Aminopyrine N-Demethylase / Q000378:metabolism*; D000818:Animals; D003577:Cytochrome P-450 Enzyme System / Q000096:biosynthesis*; D004790:Enzyme Induction; D007122:Immunoelectrophoresis; D008297:Male; D008745:Methylation; D008862:Microsomes, Liver / Q000187:drug effects* / Q000201:enzymology; D010634:Phenobarbital / Q000031:analogs & derivatives; D051381:Rats; D011919:Rats, Inbred Strains; D012521:Sarcosine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology
D000632:Aminopyrine; C025231:sarkosyl; D003577:Cytochrome P-450 Enzyme System; D000633:Aminopyrine N-Demethylase; D010634:Phenobarbital; D012521:Sarcosine