利莫那班的药理学研究进展  

Advance in the pharmacological study of rimonabant

作　　者：原野[1] 吴纯启[1] 廖明阳[1] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850

出　　处：《中国新药杂志》2009年第21期2028-2031,2092,共5页Chinese Journal of New Drugs

基　　金：重大新药创制科技重大专项(2008ZX09305-003);北京市自然科学基金(7092079);国家973课题基金(2006CB705600)

摘　　要：内源性类大麻素样物质及其受体即内源性类大麻素系统(ECS)参与生物体的能量内平衡,糖类、脂肪代谢及体重控制;而利莫那班(rimonabant)为首个大麻素Ⅰ型受体拮抗剂类强效减肥药,通过ECS发挥其减肥作用。文中扼要综述了利莫那班作用靶标大麻素受体及内源性类大麻素系统的生理作用,利莫那班的临床前药效学研究、药理作用机制、药动学和代谢以及毒性与药理作用的相互关系,并简要介绍了第二代Ⅰ型大麻素受体拮抗剂它拉那班(taranabant)的药理、药效学研究概况,以期促进安全、高效的大麻素Ⅰ型受体拮抗剂的开发。The endocannabinoid system （ECS） is consisted of endogenous cannabinoid substances and their receptors. ECS is involved in the energy homeostasis, the metabolic regulations of sugars and lipids, and the body weight control. Rimonabant is the first cannabinoid receptor Ⅰ antagonist as a weight-reducing drug, which executes pharmacological effects by the modulation of ECS. In this article, we reviewed the physiology of cannabinoid receptor and the endogenous cannabinoid system, and the preclinical pharmacodynamics, pharmacological mechanisms, pharmacokinetics and metabolisms of rimonabant. We also introduced the relationship between the toxicity and the pharmacological actions of rimonabant, and the pharmacodynamics and pharmacological actions of taranabant, a second generation cannabinoid receptor Ⅰ antagonist. We hope to facilitate the development of more safe and effective cannabinoid receptor Ⅰ antagonists.

关 键 词：利莫那班 主要药效学 作用机制 内源性大麻素系统 它拉那班 

分 类 号：R969[医药卫生—药理学]