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Drinabant
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Drinabant图片
CAS NO:358970-97-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
AVE1625
产品介绍
Drinabant (AVE1625) 是具有口服活性的CB1 受体的拮抗剂。Drinabant (AVE1625) 抑制hCB1-R 和 rCB1-R 激动剂刺激的钙信号的IC50值分别为 25 nM 和 10 nM。对 hCB2-R 无活性。
生物活性

Drinabant (AVE1625) is an orally activeCB1receptorantagonist. Drinabant (AVE1625) inhibits the agonist-stimulated calcium signal withIC50values of 25 nM and 10 nM for the hCB1-R and rCB1-R, respectively, and is ineffective for the hCB2-R[1].

IC50& Target[1]

hCB1-R

25 nM (IC50)

rCB1-R

10 nM (IC50)

CB2

10000 nM (IC50)

体内研究
(In Vivo)

AVE1625 (10 mg/kg orally once daily), combined with Olanzapine (HY-14541) attenuates body weight gain, diminishing the enhanced food intake while maintaining increased energy expenditure and decreased motility[2].
AVE1625 (1, 3, and 10 mg/kg ip), reverses abnormally persistent LI induced by MK-801 (HY-15084B) or neonatal nitric oxide synthase inhibition in rodents, and improves both working and episodic memory[3].

Animal Model:Rats[1].
Dosage:30 mg/kg.
Administration:Oral gavage, single dose.
Result:Had free access to food during the preceding night (postprandial state) caused a pronounced reduction of food intake during the subsequent 10-12 h without differences in their locomotor activity relative to that of the control group.
Caused an increase in FFA and glycerol, indicating increased lipolysis from fat tissue.
Immediately resulted in a pronounced increase in VCO2and VO2, indicating increased oxidation of energetic substrates and increased TEE.
Animal Model:Female Hanover Wistar rats weighing 225 ± 8.6 g[2].
Dosage:10 mg/kg.
Administration:Orally once daily.
Result:Reduced their weight markedly within the first 3 days of treatment where upon animals maintained lower body weight, although they lost about 7.3 ± 1.3 g fat during the 12 days of treatment.
Clinical Trial
分子量

497.38

Formula

C23H20Cl2F2N2O2S

CAS 号

358970-97-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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