RT Journal Article
SR Electronic
T1 Biotransformation of azapetine to oxazapetine in rat and rabbit liver fractions.
JF Drug Metabolism and Disposition
JO Drug Metab Dispos
FD American Society for Pharmacology and Experimental Therapeutics
SP 204
OP 207
VO 7
IS 4
A1 P C Ruenitz
A1 T P McLennon
A1 L A Sternson
YR 1979
UL http://dmd.aspetjournals.org/content/7/4/204.abstract
AB The biotransformation of azapetine (I) to a lactam metabolite, oxazapetine (II), has been investigated in rat and rabbit hepatic subcellular fractions. In the presence of NADPH, II was produced from I in incubation mixtures containing 9000 g supernatant fraction or combined microsomes and cytosol, but not in mixtures containing microsomes or cytosol alone. Production of II was also observed when dehydrozapetine (III) was incubated with rabbit 9000 g supernatant fraction or cytosol. In washed rabbit microsomes II was not produced from III, but I was converted to III in the presence of NADPH. These results suggested that the biotransformation is initiated by microsomal enzymatic oxidation of I to III, followed by further oxidation of III to II by a soluble enzyme.