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首页> 外文期刊>Life sciences >HALOPERIDOL AND ITS TETRAHYDROPYRIDINE DERIVATIVE (HPTP) ARE METABOLIZED TO POTENTIALLY NEUROTOXIC PYRIDINIUM SPECIES IN THE BABOON
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HALOPERIDOL AND ITS TETRAHYDROPYRIDINE DERIVATIVE (HPTP) ARE METABOLIZED TO POTENTIALLY NEUROTOXIC PYRIDINIUM SPECIES IN THE BABOON

机译：氟哌啶醇及其四氢吡啶衍生物（HPTP）已被代谢为狒狒中潜在的神经氧化性吡啶类

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摘要

The in vivo metabolic fate of haloperidol (HP) and its tetrahydropyridine analog HPTP have been examined in the baboon to investigate the formation of potentially neurotoxic pyridinium metabolites that have been observed previously in humans. Urine samples collected from baboons treated with HPTP were shown to contain, in addition to the parent drug, the corresponding reduced HPTP (RHPTP), generated by reduction of the butyrophenone carbonyl group. RHPTP was characterized by comparison with a synthetic standard using HPLC with electrochemical detection and HPLC/MS/MS. Another compound identified by LC/MS/MS was a glucuronide metabolite of RHPTP. The HP pyridinium (HPP+) and reduced pyridinium (RHPP(+)) metabolites were shown to be present in urine from both HP and HPTP treated baboons by HPLC using fluorescence detection. The urinary excretion profile of HPP+ and RHPP(+) in both groups was essentially identical and, in contrast to that observed in rodents, closely paralleled the profile found in humans treated with HP. These data in the baboon suggest that the metabolic processes involved in the production of the pyridinium metabolites of HP are similar to those in humans. Furthermore, the HPTP-treated baboon may be an appropriate model in which to study the role of pyridinium metabolites in the induction of tardive dyskinesia. [References: 26]
机译：已经在狒狒中检查了氟哌啶醇（HP）及其四氢吡啶类似物HPTP的体内代谢命运，以研究先前在人类中观察到的潜在神经毒性吡啶鎓代谢物的形成。除母体药物外，从用HPTP处理过的狒狒收集的尿液样品中还显示出通过还原丁苯酮羰基而产生的相应还原HPTP（RHPTP）。通过使用带有电化学检测的HPLC和HPLC / MS / MS与合成标准品进行比较，对RHPTP进行了表征。 LC / MS / MS鉴定的另一种化合物是RHPTP的葡糖苷酸代谢物。通过使用荧光检测的HPLC，HP和HPTP处理的狒狒的尿液中均存在HP吡啶鎓（HPP +）和还原吡啶鎓（RHPP（+））代谢产物。两组中HPP +和RHPP（+）的尿排泄情况基本相同，并且与啮齿类动物观察到的情况相反，这与用HP治疗的人的排泄情况非常相似。狒狒中的这些数据表明，HP的吡啶鎓代谢产物产生所涉及的代谢过程与人类相似。此外，HPTP处理的狒狒可能是一个合适的模型，用于研究吡啶鎓代谢物在诱导迟发性运动障碍中的作用。 [参考：26]

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