奥替那班

中文名称:

奥替那班

中文同义词:

1-[9-(4-氯苯基)-8-(2-氯苯基)-9H-嘌呤-6-基]-4-乙基氨基哌啶-4-甲酰胺;奥替那班

英文名称:

Otenabant

英文同义词:

otenabant;1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxamide;Otenabant (CP-945,598);Otenabant, >=98%;CP945598 free base;Otenabant (CP-945598 free base);CS-1072;CP 945598; CP-945598; CP945598

CAS号:

686344-29-6

分子式:

C25H25Cl2N7O

分子量:

510.42

EINECS号:

相关类别:

G蛋白偶联受体G蛋白;医药

Mol文件:

686344-29-6.mol

沸点 

757.9±70.0 °C(Predicted)

密度 

1.46

酸度系数(pKa)

16.30±0.20(Predicted)

生物活性

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

靶点

Ki: 0.7 nM (CB1)

体外研究

Otenabant HCl has low affinity with K i 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.

体内研究

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.