Drinabant

BeschreibungThe central cannabinoid (CB1) receptor is a G protein-coupled receptor that is widely distributed in the central nervous system and several peripheral tissues and binds the active component of cannabis, Δ9-tetrahydrocannabinol. Signaling through the CB1 receptor is implicated in attentional and working memory deficits as well as obesity. AVE-1625 is a highly potent, selective antagonist for the CB1 receptor with Ki values of 0.16-0.44 nM. At 1-3 mg/kg, AVE-1625 significantly improves the performance of rodents in working memory tasks. At 30 mg/kg, AVE-1625 reduces caloric intake by more than 50% of controls and significantly increases lipolysis from fat tissues and reduces hepatic glycogen levels in rodents.