Wood C L, Gandolfi A J, Van Dyke R A
Drug Metab Dispos. 1976 Jul-Aug;4(4):305-13.
Incubation of rat liver microsomes with 14C-halothane in a nitrogen atmosphere results in a high correlation between the formation of conjugated dienes and the binding of a halothane metabolite to phospholipids. Both the binding and the formation of the conjugated dienes required NADPH, were inhibited by carbon monoxide, and increased with duration of incubation and with protein concentration. Both [36Cl] halothane and [14C] halothane showed a similar pattern of binding to microsomal phospholipids suggesting that the chlorine atom is retained by the metabolite that binds. Neither high levels of conjugated dienes produced by halothane in microsomes incubated under nitrogen nor the binding of the halothane metabolite results in the destruction of cytochrome P-450.
在氮气环境中，用14C-氟烷孵育大鼠肝脏微粒体，结果显示共轭二烯的形成与氟烷代谢产物与磷脂的结合之间存在高度相关性。共轭二烯的结合和形成均需要NADPH，一氧化碳可抑制二者，且随着孵育时间和蛋白质浓度的增加而增加。[36Cl]氟烷和[14C]氟烷与微粒体磷脂的结合模式相似，表明结合的代谢产物保留了氯原子。在氮气环境下孵育的微粒体中，氟烷产生的高水平共轭二烯以及氟烷代谢产物的结合均不会导致细胞色素P-450的破坏。
