Is it time for cannabinoid antagonists?
One of the recent remarkable events in therapeutic neuroscience has been the approval of rimonabant, the first cannabinoid receptor Type 1 antagonist used by the European Union (EU) for treatment of obesity, hyperlipidemia, and glucose intolerance. This achievement was preceded by decades of intense scientific work on the cannabinoid field. This has led to the identification and cloning of two specific receptor types, the characterization of endogenous ligands, and the synthesis of numerous antagonists and agonists. Patents are now held on over 100 cannabinoid CB-1 (CB-1) antagonists. Preclinical studies indicate that CB-1 receptor antagonists have major modulating effects on natural reinforcers, such as food and addictive drugs such as cocaine, opiates, nicotine, and alcohol. Peripheral effects of CB-1 antagonists include increased thermogenesis, increased peripheral lipogenesis, and improvement in glycemic utilization. The treatment potential for addictive disorders, obesity, and the