Korpi E R, Wyatt R J
Psychopharmacology (Berl). 1984;83(1):34-7. doi: 10.1007/BF00427418.
Acute injection of rats with either haloperidol or reduced haloperidol (1 mg/kg, IP) greatly increased the striatal concentrations of the acidic dopamine metabolites, indicating enhanced turnover of dopamine. The effect of reduced haloperidol was almost as great as that of haloperidol. Reduced haloperidol, however, was much less efficient (about 400 times) than haloperidol in displacing [3H]spiperone binding to striatal membranes in vitro. In agreement with the above results, reduced haloperidol was found to be oxidized to haloperidol, so that 2 h after injection of reduced haloperidol the concentrations of haloperidol and reduced haloperidol were equal in the striatum. The apparent conversion of reduced haloperidol to haloperidol was much quicker in liver than in plasma or brain, and it is suggested that the conversion primarily occurs in the liver. Before drawing any definite conclusion about the possible central activity of reduced haloperidol, further studies with other animal species are needed.
给大鼠腹腔注射氟哌啶醇或还原氟哌啶醇（1毫克/千克）后，大鼠纹状体中酸性多巴胺代谢产物的浓度大幅增加，这表明多巴胺的周转率提高。还原氟哌啶醇的作用几乎与氟哌啶醇相同。然而，在体外，还原氟哌啶醇取代纹状体膜上[3H]螺哌隆结合的效率比氟哌啶醇低得多（约400倍）。与上述结果一致，发现还原氟哌啶醇被氧化为氟哌啶醇，因此在注射还原氟哌啶醇2小时后，纹状体中氟哌啶醇和还原氟哌啶醇的浓度相等。还原氟哌啶醇向氟哌啶醇的表观转化在肝脏中比在血浆或大脑中快得多，提示这种转化主要发生在肝脏。在对还原氟哌啶醇可能的中枢活性得出任何明确结论之前，还需要对其他动物物种进行进一步研究。
