Advance in the pharmacological study of rimonabant
YUAN Ye
WU Chun-qi
LIAO Ming-yang
Abstract：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 tar-anabant, a second generation cannabinoid receptor Ⅰ antagonist. We hope to facilitate the development of more safe and effective cannabinoid receptor Ⅰ antagonists.
Keywords：rimonabantprimary pharmacodynamicsmechanismsendogenous cannabinoid systemtaranabant
Publication Date：2009-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：5( 2028-2031,2092 )