1. GPCR/G Protein
    Neuronal Signaling
  2. Cannabinoid Receptor
  3. Drinabant

Drinabant (Synonyms: AVE1625)

Cat. No.: HY-14788
Handling Instructions

Drinabant (AVE1625) is an orally active CB1 receptor antagonist. Drinabant (AVE1625) 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.

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Drinabant Chemical Structure

Drinabant Chemical Structure

CAS No. : 358970-97-5

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Description

Drinabant (AVE1625) is an orally active CB1 receptor antagonist. Drinabant (AVE1625) 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[1].

IC50 & Target[1]

hCB1-R

25 nM (IC50)

rCB1-R

10 nM (IC50)

CB2

10000 nM (IC50)

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 VCO2 and 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.
Molecular Weight

497.38

Formula

C₂₃H₂₀Cl₂F₂N₂O₂S

CAS No.

358970-97-5

SMILES

CS(=O)(N(C1CN(C(C2=CC=C(Cl)C=C2)C3=CC=C(Cl)C=C3)C1)C4=CC(F)=CC(F)=C4)=O

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Storage

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

References
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Keywords:

DrinabantAVE1625AVE 1625AVE-1625Cannabinoid ReceptorOlanzapineweightgainfoodintakeepisodicmemoryInhibitorinhibitorinhibit

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