Peripheral CNR1 antagonists to the fore
In the three years following an FDA panel recommendation against approval of sanofi-aventis Group's Acomplia rimonabant to treat obesity due to severe neurological side effects, centrally acting inhibitors of
cannabinoid CB1 receptor have all but disappeared from development. Now, researchers at the NIH and Northeastern University have taken the CNS out of the equation by showing that a peripheral inhibitor of the receptor treated obesity and related metabolic disorders without eliciting neurological side effects in mice even though it could not enter the CNS.1
The NIH group is now working with Jenrin Discovery Inc., which has a number of peripheral cannabinoid CB1 receptor (CNR1) inhibitors in preclinical development. The company hopes to select a lead compound to treat diabetes or liver disease.
CNR1 is expressed in the brain,