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) |
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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.
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| 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. |
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