Otenabant 是选择性 Cannabinoid Receptor CB1拮抗剂，Ki=0.7 nM，对其选择性是对 CB2 的 1000 多倍。

Otenabant has been investigated for the treatment of Obesity.

Otenabant HCl has a low Ki affinity for human CB2 receptors of 7.6 μM[1]. Otenabant HCl inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration[2].

Otenabant acutely stimulates energy expenditure in rats and decreases the respiratory quotient which suggests a metabolic switch to increased fat oxidation. Otenabant (10 mg/kg, p.o.) promotes a 9%, vehicle-adjusted weight loss in a 10-day weight loss study in diet-induced obese mice[1]. Otenabant HCl reverses four cannabinoid agonist-mediated behaviors (locomotor activity, hypothermia, analgesia, and catalepsy) following administration of the synthetic CB1 receptor agonist CP-55940. Otenabant HCl exhibits dose-dependent anorectic activity in a model of acute food intake in rodents and increased energy expenditure and fat oxidation[2].

686344-29-6

C25H25Cl2N7O

510.42

奥替那班;CP-945598

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years