Drinabant

Research use only, not for human use.

Drinabant is an orally active CB1 receptor antagonist. Drinabant inhibits the agonist-stimulated calcium signal with IC50 values of 25 nM and 10 nM for the hCB1-R and rCB1-R, respectively, and is ineffective for the hCB2-R.

Drinabant is an orally active CB1 receptor antagonist. Drinabant inhibits the agonist-stimulated calcium signal with IC50 values of 25 nM and 10 nM for the hCB1-R and rCB1-R, respectively, and is ineffective for the hCB2-R.(In Vivo):Drinabant (10 mg/kg orally once daily), combined with Olanzapine attenuates body weight gain, diminishing the enhanced food intake while maintaining increased energy expenditure and decreased motility. Drinabant (1, 3, and 10 mg/kg ip), reverses abnormally persistent LI induced by MK-801 or neonatal nitric oxide synthase inhibition in rodents, and improves both working and episodic memory.

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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. 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. Animal Model:Rats.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 intheir 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 VCO2 and VO2, indicating increased oxidation of energetic substrates and increased TEE.Animal Model:Female Hanover Wistar rats weighing 225 ± 8.6 g.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.

AVE-1625

GPCR/G Protein

Cannabinoid Receptor

TRPV1

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358970-97-5

497.39

C23H20Cl2F2N2O2S

>98% (HPLC)

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CS(N(C(C1)CN1C(c(cc1)ccc1Cl)c(cc1)ccc1Cl)c1cc(F)cc(F)c1)(=O)=OCS(N(C(C1)CN1C(c(cc1)ccc1Cl)c(cc1)ccc1Cl)c1cc(F)cc(F)c1)(=O)=O

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(-20℃)

With Ice Pack

≥ 2 years