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利莫那班(rimonabant)为首个大麻素Ⅰ型受体(CB1)抑制剂类减肥药,有很好的减肥效果。但近期的研究表明利莫那班可增加抑郁、焦虑、自杀等严重精神不良反应的发生率。文中扼要综述了利莫那班在次要药效学和安全性药理学、一般毒性、毒性靶器官系统、遗传毒性、致癌性和生殖毒性以及刺激性、依赖性等方面的临床前毒理学特征,以促进具有更高安全性的大麻素Ⅰ型受体拮抗剂的开发。
Rimonabant (rimonabant) is the first anti-obesity drug of type CB1 inhibitor, which has a good weight-loss effect. However, recent studies have shown that rimonabant can increase the incidence of serious adverse mental reactions such as depression, anxiety and suicide. This review summarizes the preclinical toxicological profile of rimonabant in terms of secondary pharmacodynamics and safety pharmacology, general toxicity, toxic target organ systems, genotoxicity, carcinogenicity and reproductive toxicity as well as irritation and dependence , To promote the development of cannabinoid type 1 receptor antagonists with greater safety.