Bellward G D, Li M, Lopaschuk G D, Warren P
Res Commun Chem Pathol Pharmacol. 1977 Nov;18(3):415-22.
Male and female Wistar rats were administered alpha-1-acetylmethadol via their drinking water for one to two weeks. Hepatic aryl hydrocarbon hydroxylase, cytochrome P-450 and epoxide hydrase activities were measured after various doses of this drug. In female rats, a significant increase in aryl hydrocarbon hydroxylase and cytochrome P-450 occurred at doses as low as 4.7 mg/Kg/day. However, no change in epoxide hydrase activity occurred. In male rats, a significant increase in epoxide hydrase activity occurred at all doses tested. From these results, it is concluded that alpha-1-acetylmethadol induces a number of hepatic drug metabolizing enzyme systems.
将雄性和雌性Wistar大鼠通过饮用水给予α-1-乙酰美沙醇,持续一至两周。在给予该药物不同剂量后,测定肝芳烃羟化酶、细胞色素P-450和环氧化物水解酶的活性。在雌性大鼠中,低至4.7毫克/千克/天的剂量时,芳烃羟化酶和细胞色素P-450就出现显著增加。然而,环氧化物水解酶活性没有变化。在雄性大鼠中,所有测试剂量下环氧化物水解酶活性均出现显著增加。从这些结果可以得出结论,α-1-乙酰美沙醇可诱导多种肝药物代谢酶系统。