Otenabant

Otenabant HCl has low affinity with K _i of 7.6 μM for human CB2 receptors. It inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration. < /p>

Otenabant acutely stimulates energy expenditure in rats and decreases the respiratory quotient indicating a metabolic switch to increased fat oxidation. It (10 mg/kg, po) promotes a 9%, vehicle adjusted weight loss in a 10 day weight loss study in diet-induced obese mice. Otenabant HCl reverses four cannabinoid agonistmediated behaviors (locomotor activity, hypothermia, analgesia, and catalepsy) following administration of the synthetic CB1 receptor agonist CP-55940. And Otenabant HCl exhibits dose-dependent anorectic activity in a model of acute food intake in rodents and increased energy expenditure and fat oxidation.

Ki: 0.7 nM (CB1)