Advance in the pharmacological study of rimonabant

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 receptorⅠantagonist 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 receptorⅠantagonist.We hope to facilitate the development of more safe and effective cannabinoid receptorⅠantagonists.