CP 945598 hydrochloride

CP 945598 hydrochloride (Otenabant HCl) is a potent and selective cannabinoid type 1 receptor antagonist that inhibits both basal and cannabinoid agonist-mediated CB(1) receptor signaling in vitro and in vivo. It displays low affinity for human CB2 receptors with Ki of 7600 nM. In vivo, CP-945598 reversed cannabinoid agonist-mediated responses, reduced food intake, and increased energy expenditure and fat oxidation in rodents. CP 945598 exhibits dose and concentration-dependent anorectic activity in two models of acute food intake in rodents, fast-induced re-feeding and spontaneous, nocturnal feeding. CP-945598 also acutely stimulates energy expenditure in rats and decreases the respiratory quotient indicating a metabolic switch to increased fat oxidation.