Ruenitz P C, McLennon T P, Sternson L A
Drug Metab Dispos. 1979 Jul-Aug;7(4):204-7.
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.
已在大鼠和兔肝脏亚细胞组分中研究了氮杂etine（I）向一种内酰胺代谢物恶唑etine（II）的生物转化。在存在NADPH的情况下，在含有9000g上清液组分或混合微粒体与胞质溶胶的孵育混合物中，II由I产生，但在仅含微粒体或胞质溶胶的混合物中则不会产生。当脱氢氮杂etine（III）与兔9000g上清液组分或胞质溶胶一起孵育时，也观察到了II的产生。在洗涤过的兔微粒体中，III不会产生II，但在存在NADPH的情况下，I会转化为III。这些结果表明，生物转化是由微粒体酶将I氧化为III开始的，随后由一种可溶性酶将III进一步氧化为II。
