外周型Ⅰ型大麻素受体选择性拮抗剂的研究进展  

Peripherally restricted CB1 receptor antagonist:research advances

作　　者：税凤春 陈伟[2] 徐静华[1] 王莉莉[2] 

机构地区：[1]沈阳药科大学生命科学与生物制药学院,沈阳110016 [2]军事医学科学院毒物药物研究所,北京100850

出　　处：《国际药学研究杂志》2014年第5期552-558,共7页Journal of International Pharmaceutical Research

基　　金：国家"重大新药创制"科技重大专项资助项目(2012ZX09301003-001;2012ZX09301003-003);国家自然科学基金资助项目(81102308)

摘　　要：Ⅰ型大麻素受体(cannabinoid 1 receptor,CB1R)是肥胖症治疗药物研发的最重要靶标之一,然而以利莫那班为代表的CB1R拮抗剂因中枢作用产生的副作用限制了其临床应用。不透过血脑屏障的外周型CB1R选择性拮抗剂在保留第1代CB1R拮抗剂减肥效应的同时,避免了其中枢相关的副作用,成为当前CB1R拮抗剂类新型减肥药物研发的方向。本文综述了外周型CB1R选择性拮抗剂的研究进展。Cannabinoid 1 receptor（CB1R） is one of most important targets for the treatment of obesity. However, the clinical application of CB1 R antagonist rimonabant is restricted because of the central nervous system-related unwanted liabilities.Peripherally restricted CB1 R antagonist with limited blood-brain-barrier penetration may maintain the antiobesity efficacy of rimonabant without unwanted side effects. This strategy has become the new hot spot for the development of antiobesity drugs. In this paper, we review the recent progress in peripherally restricted CB1 receptor antagonist.

关 键 词：外周选择性 Ⅰ型大麻素受体 拮抗剂 血脑屏障 

分 类 号：R96[医药卫生—药理学]