Abstract：
Risperidone (Ris) is a second-generation antipsychotic that belongs to the chemical class of benzisoxazole derivatives. 9-Hydroxy (9OH-) Ris is well known among the six reported metabolites of Ris and had been examined using not only blood but also other matrices, but the other five metabolites reported such as benzisoxazole ring-cleaved Ris (c-Ris) and c-9OH-Ris had been detected only in blood, urine and feces. In the present work, large peaks of c-Ris and c-9OH-Ris were detected in the liver, kidney, cerebrum, blood, pericardial fluid, bile and urine obtained from two cadavers. There is a potential that c-Ris and c-9OH-Ris will be good markers to prove Ris consumption in forensic toxicology cases. For example, the peak ratios of c-Ris against the parent Ris in the kidney and blood were as high as 3.9 and 3.6 in cadaver 1; and 7.0 and 7.9 in cadaver 2, respectively. In addition to the previously reported six metabolites, five new metabolites such as dehydrogenated-Ris, 7-keto-Ris and three benzisoxazole ring-cleaved metabolites were disclosed in the present work, and the pathways for the totally eleven metabolites detected in human solid tissues and body fluids have also been proposed, because such pathways were neither reported nor discussed previously.
摘要：
利培酮（Ris）是第二代抗精神病药，属于苯并异恶唑衍生物的化学类别。9-羟基（9OH-）Ris在已报道的六种Ris代谢物中是众所周知的，并且不仅使用血液而且还使用其他基质进行了检查。但是报告的其他五种代谢物，如苯并异恶唑环裂解的Ris（c-Ris）和c-9OH-Ris，仅在血液中检测到，尿液和粪便。在目前的工作中,在肝脏中检测到c-Ris和c-9OH-Ris的大峰，肾,大脑,血,心包液,从两具尸体中获得的胆汁和尿液。在法医毒理学案例中，c-Ris和c-9OH-Ris可能是证明Ris消耗的良好标记。例如,肾脏和血液中c-Ris与亲本Ris的峰值比率在尸体1中分别高达3.9和3.6；尸体2中分别为7.0和7.9。除了先前报道的六种代谢物，五种新的代谢物，如脱氢-Ris，在本工作中公开了7-酮-Ris和三种苯并异恶唑环裂解的代谢物，并且还提出了在人体固体组织和体液中检测到的总共11种代谢物的途径，因为以前既没有报道也没有讨论过这种途径。
