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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。
Endogenous cannabinoid-like substances and their receptors, the endogenous cannabinoid system (ECS), are involved in the energy homeostasis, carbohydrate, fat metabolism, and body weight control of organisms; and rimonabant is the first Cannabinoid type I receptor antagonist potent diet pills, through the ECS to play its role in weight loss. In this review, we summarize the physiological roles of rimonabant, a target cannabinoid receptor, and the endocannabinoid system, preclinical pharmacodynamics, pharmacological mechanisms, pharmacokinetics and metabolism, and toxicity of rimonabant and Pharmacological effects of the second generation of the type I cannabinoid receptor antagonist itranabant (taranabant) pharmacological and pharmacodynamic profiles, with a view to promoting safe and efficient cannabinoid type 1 receptor antagonism Agent development.