Rimonabant, also known as SR141716, was the first selective central cannabinoid (CB1) receptor inverse agonist (Ki = 1.8 nM) to be developed as an appetite suppressant, anti-obesity drug. Rimonabant is widely used as a tool to investigate CB receptor properties and the mechanisms by which CB agonists exert their pharmacological effects. In rodent models and clinical trials, rimonabant effectively induces lipolysis, reduces hepatomegaly, decreases body weight, and improves dyslipidemia by reducing triglyceride, free fatty acid, and total cholesterol levels and by increasing HDL/LDL ratios.