In vitro studies on irreversible binding of halothane metabolite to microsomes

Incubation of rat liver microsomal suspensions with [14C] halothane resulted in the binding of a metabolite of halothane to microsomal phospholipids and, to a lesser extent, to microsomal proteins. The binding was inhibited by carbon monoxide, required NADPH, and was greatly enhanced under anaerobic conditions. The binding to lipids occurred only to phospholipids, particularly those with characteristics of phosphatidylcholine and phosphatidylethanolamine. The binding was dependent on the time of incubation as well as on the amount of microsomes present.