大麻受体1阻滞剂的构效关系研究进展

Progresses in the investigations of cannabinoid receptor-1(CB_1-R) antagonists

大麻受体1(CB1-R)属于G-蛋白耦联受体超家族成员,主要分布于中枢神经系统。选择性的CB1受体阻滞剂通过作用该受体,具有治疗肥胖、酒精依赖、尼古丁成瘾、认知障碍以及胃肠道系统疾病等作用。目前,已发现有许多二芳基吡唑类和基于此类化合物衍生出来的多种类型化合物表现出较高的选择性和较好的阻断活性。现综述该类药物的作用机制、结构修饰和构效关系。

Cannabinoid receptor-1 （CB1-R） is one of the G-protein coupled receptors, and it is expressed predominantly in the central nervous system. Selective CB1-R antagonists have potential in the treatment of a number of diseases, such as obesity, alcohol dependence, nicotine addiction, cognitive disorders, and gastrointestinal disorders. Recent studies found that many diphenylpyrazoles and other derivated compounds have good CBj-R selectivity and antagonistic activity. In this review, the mechanism, structural modifications and structure-activity relationship of CB1-R antagonists are summarized.