Otenabant 是一种有效的，选择性的 cannabinoid receptor CB1 拮抗剂，K_i 值为 0.7 nM，对其选择性是对 CB2 的 1000 多倍。

Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with K i of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.

Solid

Ki: 0.7 nM (CB1)

Otenabant HCl has low affinity with Ki of 7.6 μM for human CB2 receptors. Otenabant HCl inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration. has not independently confirmed the accuracy of these methods. They are for reference only.

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. 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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. John R. Hadcock, et al. In vitro and in vivo pharmacology of CP-945,598, a potent and selective cannabinoid CB1 receptor antagonist for the management of obesity. Biochemical and Biophysical Research Communications, 2010; 394;366-371.
[2]. Griffith DA, et al. Discovery of 1-[9-(4-chlorophenyl) -8-(2-chlorophenyl)- 9H-purin-6-yl] -4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. JMedChem. 2009 ;5

In Vitro: DMSO : 100 mg/mL (195.92 mM; Need ultrasonic)配制储备液