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AVE-1625 Exclusive

Cayman Chemical Item Number 10009021

(CAS 358970-97-5)

AVE-1625 (CAS 358970-97-5)

See more	Receptor Antagonist (45) Alzheimer's Research (44) Metabolism (139) Neuroscience (654) Obesity (162) Parkinson's Research (18)

Description

The central cannabinoid (CB₁) receptor is a G protein-coupled receptor that is widely distributed in the central nervous system and several peripheral tissues and binds the active component of cannabis, Δ⁹-tetrahydrocannabinol.¹ Signaling through the CB₁ receptor is implicated in attentional and working memory deficits as well as obesity.^2,3,4 AVE-1625 is a highly potent, selective antagonist for the CB₁ receptor with K_i values of 0.16-0.44 nM.⁴ At 1-3 mg/kg, AVE-1625 significantly improves the performance of rodents in working memory tasks.⁴ At 30 mg/kg, AVE-1625 reduces caloric intake by more than 50% of controls and significantly increases lipolysis from fat tissues and reduces hepatic glycogen levels in rodents.⁵

1 Howlett, A.C., Song, C., Berglund, B.A., et al. Characterization of CB₁ cannabinoid receptors using receptor peptide fragments and site-directed antibodies. Mol Pharmacol 53 504-510 (1998).

2 Gómez, R., Navarro, M., Ferrer, B., et al. A peripheral mechanism for CB₁ cannabinoid receptor-dependent modulation of feeding. J Neurosci 22(21) 9612-9617 (2002).

3 Mackie, K. Cannabinoid receptors as therapeutic targets. Annu Rev Pharmacol Toxicol 46 101-122 (2006).

4 Borowsky, B., Stevens, R., Mark, B., et al. AVE1625, a cannabinoid CB₁ antagonist, as a co-treatment for Schizophrenia: Improvement in cognitive function and reduction of antipsychotic-side effects in animal models. Neuropsychopharmacology 30 S77-S142 (2005).

5 Herling, A.W., Gossel, M., Haschke, G., et al. The CB₁ receptor antagonist AVE1625 affects primarily metabolic parameters independently of reduced food intake in wistar rats. Am J Physiol Endocrinol Metab 293 E826-E832 (2007).

Formal Name	N-[1-[bis(4-chlorophenyl)methyl]-3-azetidinyl]-N-(3,5-difluorophenyl)-methanesulfonamide
CAS Number	358970-97-5
Molecular Formula	C₂₃H₂₀Cl₂F₂N₂O₂S
Formula Weight	497.4
Formulation	A crystalline solid
Purity	>98%
λ_max	231 nm
Stability	2 years
Storage	-20°C
Shipping	Room temperature in continental US; may vary elsewhere
SMILES	Copy SMILES to clipboard Clc1ccc(cc1)C(c1ccc(Cl)cc1)N1CC(C1)N(c1cc(F)cc(F)c1)S(=O)(=O)C

Background Reading

Mackie, K. Cannabinoid receptors as therapeutic targets. Annu Rev Pharmacol Toxicol 46 101-122 (2006).

Howlett, A.C., Song, C., Berglund, B.A., et al. Characterization of CB₁ cannabinoid receptors using receptor peptide fragments and site-directed antibodies. Mol Pharmacol 53 504-510 (1998).

Herling, A.W., Gossel, M., Haschke, G., et al. The CB₁ receptor antagonist AVE1625 affects primarily metabolic parameters independently of reduced food intake in wistar rats. Am J Physiol Endocrinol Metab 293 E826-E832 (2007).

Borowsky, B., Stevens, R., Mark, B., et al. AVE1625, a cannabinoid CB₁ antagonist, as a co-treatment for Schizophrenia: Improvement in cognitive function and reduction of antipsychotic-side effects in animal models. Neuropsychopharmacology 30 S77-S142 (2005).

Gómez, R., Navarro, M., Ferrer, B., et al. A peripheral mechanism for CB₁ cannabinoid receptor-dependent modulation of feeding. J Neurosci 22(21) 9612-9617 (2002).

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Size	Price	Quantity	Subtotal
1 mg	$49.00		$0.00
5 mg	$221.00		$0.00
10 mg	$392.00		$0.00
50 mg	$1,715.00		$0.00
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-02-12. Prices are subject to change without notice.

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