期刊
BRITISH JOURNAL OF PHARMACOLOGY
卷 152, 期 5, 页码 565-566出版社
WILEY
DOI: 10.1038/sj.bjp.0707349
关键词
cannabinoid; CB1 receptor; appetite; allosteric; anandamide; 2-AG
Cannabinoid CB1 receptor antagonists are novel therapeutics with potential for the treatment of a number of conditions including obesity, nicotine addition and metabolic syndrome. In 2005, Price et al. demonstrated that the cannabinoid CB1 receptor contains an allosteric-binding site which binds synthetic small molecules. In this issue of the British Journal of Pharmacology, Horswill et al. have extended these observations. They demonstrate that a structurally similar small molecule allosterically modulates the cannabinoid CB1 receptor and reduces body weight and food intake in an acute feeding model. Allosteric modulation now contends as a new strategy in the therapeutic exploitation of cannabinoid receptors that may offer certain advantages over the more familiar small molecules targeting the orthosteric site.
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