Tuning the endocannabinoid system: allosteric modulators of the CB1 receptor.
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.
Ross
R A
RA
School of Medical Science, Institute of Medical Sciences, University of Aberdeen, Aberdeen, Scotland, UK. r.ross@abdn.ac.uk
D000494:Allosteric Regulation / Q000187:drug effects; D000818:Animals; D001835:Body Weight / Q000187:drug effects; D063385:Cannabinoid Receptor Modulators / Q000494:pharmacology*; D004435:Eating / Q000187:drug effects; D063388:Endocannabinoids; D006801:Humans; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors* / Q000378:metabolism
D063385:Cannabinoid Receptor Modulators; D063388:Endocannabinoids; D043884:Receptor, Cannabinoid, CB1