Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6856-60. doi: 10.1016/j.bmcl.2011.09.016. Epub 2011 Sep 13.


Obesity remains a significant public health issue leading to Type II diabetes and cardiovascular disease. CB1 antagonists have been shown to suppress appetite and reduce body weight in animal models as well as in humans. Evaluation of pre-clinical CB1 antagonists to establish relationships between in vitro affinity and in vivo efficacy parameters are enhanced by ex vivo receptor occupancy data. Synthesis and biological evaluation of a novel and highly selective radiolabeled CB1 antagonist is described. The radioligand was used to conduct ex vivo receptor occupancy studies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Obesity Agents / chemistry*
  • Anti-Obesity Agents / pharmacology*
  • Brain / diagnostic imaging
  • Humans
  • Obesity / drug therapy
  • Radiography
  • Radioligand Assay / methods*
  • Rats
  • Receptor, Cannabinoid, CB1 / antagonists & inhibitors*
  • Receptor, Cannabinoid, CB1 / metabolism*


  • Anti-Obesity Agents
  • Receptor, Cannabinoid, CB1