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芬苯达唑的氧化代谢:一项比较研究。

The oxidative metabolism of fenbendazole: a comparative study.

作者信息

Short C R, Flory W, Hsieh L C, Barker S A

机构信息

Department of Veterinary Physiology, Pharmacology and Toxicology, School of Veterinary Medicine, Louisiana State University, Baton Rouge 70803.

出版信息

J Vet Pharmacol Ther. 1988 Mar;11(1):50-5. doi: 10.1111/j.1365-2885.1988.tb00120.x.

Abstract

The oxidative metabolism of fenbendazole (FBZ) was studied in hepatic fractions prepared from livers of cattle, sheep, goats, chickens, ducks, turkeys, rats, rabbits and catfish. All species produced the sulfoxide metabolite (oxfendazole; FBZ-SO), and p-hydroxyfenbendazole (FBZ-OH) was produced by all species except sheep. The product of demethoxycarbonylation, fenbendazole amine (FBZ-NH2), was not produced by liver preparations of any species. A fourth metabolite, resulting from the further oxidation of oxfendazole, fenbendazole sulfone (FBZ-SO2), was formed in all species but at highly varying rates. The chicken exhibited the highest overall rate of FBZ metabolism, followed by the duck, goat, sheep, steer, catfish, rat, rabbit, and turkey. Considerable variation was evident among avian species, the duck and turkey produced substantially less of the FBZ-OH and FBZ-SO2 metabolites than the chicken. Catfish liver preparations formed equivalent amounts of metabolite at 25 degrees C and 37 degrees C incubation temperatures. The formation of the sulfone metabolite (FBZ-SO2), however, was practically nonexistent in catfish.

摘要

在从牛、羊、山羊、鸡、鸭、火鸡、大鼠、兔子和鲶鱼肝脏制备的肝部分中研究了芬苯达唑(FBZ)的氧化代谢。所有物种都产生了亚砜代谢物(奥芬达唑;FBZ-SO),除绵羊外的所有物种都产生了对羟基芬苯达唑(FBZ-OH)。任何物种的肝脏制剂都未产生去甲氧羰基化产物芬苯达唑胺(FBZ-NH2)。由奥芬达唑进一步氧化产生的第四种代谢物芬苯达唑砜(FBZ-SO2)在所有物种中均有形成,但形成速率差异很大。鸡表现出最高的FBZ总体代谢速率,其次是鸭、山羊、绵羊、公牛、鲶鱼、大鼠、兔子和火鸡。禽类物种之间存在明显差异,鸭和火鸡产生的FBZ-OH和FBZ-SO2代谢物比鸡少得多。鲶鱼肝制剂在25℃和37℃的孵育温度下形成等量的代谢物。然而,鲶鱼中几乎不存在砜代谢物(FBZ-SO2)的形成。

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