利莫那班药理学研究进展.pdfVIP

Chinese Journal ofN ew Drugs 2009, 18( 21) # # , , (军事医学科学院毒物药物研究所, 北京 100850) [] 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 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( rmi onabant) 为首 个大麻素Ñ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 药理作用的相互关系, 并简要介绍了第 二代Ñ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Ñ 型受体拮抗剂的开发 [] 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 [] R969 [] A [] 1003 3734( 2009) 21 2028 05 Advance in the pharmacological study of rimonabant YUAN Y e, WU Chun q,i LIAO M ing yang (Institute of Pharmacology and Toxicology, Academy of M ilitaryM edicalSciences, Beij ing 100850, China) [Abstract] The endocannabinoid system ( ECS) is consisted of endogenous cannabinoid substances and their receptors1 ECS is involved in the energy homeostasis, the metabolic regulations of sugars and lipids, and the body weight control1 Rmi onabant is the first cannabinoid receptorÑantagonist as aweight reducing drug, which ex ecutes pharmacological effects by themodulation ofECS1 In this article, we reviewed the physiology of cannabinoid receptor and the endogenous cannabinoid system, and the preclinical pharm acodynam ics, pharmacologicalmecha nisms, pharmacokinetics andm etabolisms of rmi onabant1W e also introduced the relationship between the toxicity and the pharmacological actions of rmi onabant, and the pharm acodynam ics and pharmacological actions of tar anabant, a second generation cannabinoid receptorÑ antagonist1W e hope to facilitate the development ofmore safe and effective cannabinoid receptorÑantagonists1 [K ey words] rmi onabant; prmi ary pharmacodynam ics; m echanism s; endogenous cannabinoid system; tar anabant 60, v 9 , , , , () 20,