Tuning the endocannabinoid system: Allosteric modulators of the CB1 receptor

R. A. Ross

Research output: Contribution to journalComment/debate

17 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)565-566
Number of pages2
JournalBritish Journal of Pharmacology
Volume152
Issue number5
DOIs
Publication statusPublished - Nov 2007

Keywords

  • cannabinoid
  • CB1 receptor
  • appetite
  • allosteric
  • anandamide
  • 2-AG
  • cannabinoid receptors
  • neutral antagonism
  • inverse agonism
  • drug

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