期刊
CURRENT TOPICS IN MEDICINAL CHEMISTRY
卷 19, 期 16, 页码 1418-1435出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1568026619666190708164841
关键词
CB1 receptor; Psychiatric side effects; Neutral antagonists; Peripherally restricted antagonists; Allosteric modulators; Therapeutics development
资金
- National Institute on Drug Abuse, National Institutes of Health, USA [DA040693, DA040460, DA045910]
The Cannabinoid CB1 Receptor (CB1R) is involved in a variety of physiological pathways and has long been considered a golden target for therapeutic manipulation. A large body of evidence in both animal and human studies suggests that CB1R antagonism is highly effective for the treatment of obesity, metabolic disorders and drug addiction. however, the first-in-class CB1R antagonist/inverse agonist, rimonabant, though demonstrating effectiveness for obesity treatment and smoking cessation, displays serious psychiatric side effects, including anxiety, depression and even suicidal ideation, resulting in its eventual withdrawal from the European market. Several strategies are currently being pursued to circumvent the mechanisms leading to these side effects by developing neutral antagonists, peripherally restricted ligands, and allosteric modulators. In this review, we describe the progress in the development of therapeutics targeting the CB in the last two decades.
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