Korpi E R, Costakos D T, Wyatt R J
Acta Pharmacol Toxicol (Copenh). 1985 Feb;56(2):94-8. doi: 10.1111/j.1600-0773.1985.tb01260.x.
Haloperidol, a butyrophenone neuroleptic, is metabolically reduced in man, but not in rat and not in many other experimental animals. Here we present data that describes reductive haloperidol metabolism in guinea pigs in vivo. When haloperidol was injected intraperitoneally to guinea pigs, it was converted to reduced haloperidol so quickly that 1 hr after the injection the concentration of haloperidol was only about one fifth of that of reduced haloperidol. Dopamine metabolism was enhanced in the striatum after the administration of reduced haloperidol, but this enhancement could mostly be explained by oxidation of a small amount of reduced haloperidol back to haloperidol. The molecular mechanisms of haloperidol reduction should be further studied using guinea pigs as a model for human haloperidol metabolism.
氟哌啶醇是一种丁酰苯类抗精神病药物，在人体内会发生代谢还原，但在大鼠及许多其他实验动物体内则不会。在此，我们展示了描述豚鼠体内氟哌啶醇还原代谢的数据。当向豚鼠腹腔注射氟哌啶醇时，它会迅速转化为还原型氟哌啶醇，以至于注射后1小时，氟哌啶醇的浓度仅约为还原型氟哌啶醇浓度的五分之一。给予还原型氟哌啶醇后，纹状体中的多巴胺代谢增强，但这种增强主要可通过少量还原型氟哌啶醇氧化回氟哌啶醇来解释。应以豚鼠作为人类氟哌啶醇代谢的模型，进一步研究氟哌啶醇还原的分子机制。
