Otenabant Hydrochloride is a potent and selectivecannabinoid receptorCB1antagonist withK_iof 0.7 nM, exhibits 10,000-fold greater selectivity against humanCB2receptor.

Ki: 0.7 nM (CB1)

Otenabant HCl has low affinity with K_iof 7.6 μM for human CB2 receptors^[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 indicating 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 agonistmediated 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].

546.88

C₂₅H₂₆Cl₃N₇O

686347-12-6

奥替那班盐酸盐

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.