Rimonabant is an anorectic antiobesity drug approved in Europe in 2006 but was withdrawn worldwide in 2008 due to serious psychiatric side effects; it was never approved in the United States. Rimonabant is an inverse agonist for the cannabinoid receptor C (CB1) and binds with high affinity to central CB1 receptors to reduce appetite and modulate reward pathways; chemically it is a lipophilic, orally active pyrazole-derived antagonist/inverse agonist that undergoes extensive hepatic metabolism with multiple oxidative metabolites, displays good oral bioavailability, and has a prolonged terminal elimination phase consistent with tissue distribution and enterohepatic recycling.
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