SR141716A, A POTENT AND SELECTIVE ANTAGONIST OF THE BRAIN CANNABINOIDRECEPTOR

SR141716A is the first selective and orally active antagonist of the b rain cannabinoid receptor. This compound displays nanomolar affinity f or the central cannabinoid receptor but is not active on the periphera l cannabinoid receptor. In vitro, SR141716A antagonises the inhibitory effects of cannabinoid receptor agonists on both mouse vas deferens c ontractions and adenylyl cyclase activity in rat brain membranes. Afte r intraperitoneal or oral administration SR141716A antagonises classic al pharmacological and behavioural effects of cannabinoid receptor ago nists. This compound should prove to be a powerful tool for investigat ing the in vivo Functions of the anandamide/cannabinoid system.