Aitio M L, Aitio A
Arch Int Pharmacodyn Ther. 1979 May;239(1):16-23.
An in vitro assay for the determination of the activity of disopyramide-N-dealkylation was developed. This reaction was concluded to be catalyzed by the liver microsomal, cytochrome P-450 centered monooxygenase system. Phenobarbital enhanced the N-dealkylation of disopyramide four fold, and disopyramide itself 1.6 fold, whereas methylcholanthrene was without effect. Disopyramide also increased ethoxycoumarin deethylation 1.6 fold, and had a slight increasing effect on the activity of epoxide hydratase, but did not affect the activities of glutathione S-transferase or UDPglucuronosyltransferase.
开发了一种用于测定丙吡胺 - N - 脱烷基化活性的体外试验。该反应被认为是由肝脏微粒体中以细胞色素P - 450为中心的单加氧酶系统催化的。苯巴比妥使丙吡胺的N - 脱烷基化增强了四倍,使丙吡胺本身增强了1.6倍,而甲基胆蒽则无作用。丙吡胺还使乙氧基香豆素脱乙基化增强了1.6倍,对环氧水合酶的活性有轻微增强作用,但不影响谷胱甘肽S - 转移酶或尿苷二磷酸葡萄糖醛酸基转移酶的活性。