Drinabant - CAS 358970-97-5
Catalog number: 358970-97-5
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Cannabinoid Receptor
Drinabant is a highly potent, selective antagonist for the CB1 receptor with Ki values of 0.16-0.44 nM.
White Solid
AVE1625; AVE 1625; AVE-1625; Drinabant.N-[1-[bis(4-chlorophenyl)methyl]azetidin-3-yl]-N-(3,5-difluorophenyl)methanesulfonamide;
Soluble in DMSO
Store at -20 °C
Cannabinoid receptor CB1 antagonists
Quality Standard:
Enterprise standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly.
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1.Ligand Binding Sensitivity of the Extracellular Loop Two of the Cannabinoid Receptor 1.
Bertalovitz AC;Ahn KH;Kendall DA Drug Dev Res. 2010 Nov 1;71(7):404-411.
The cannabinoid receptor one (CB1) is a class A G-protein-coupled receptor thought to bind ligands primarily within its helical bundle. Evidence suggests, however, that the extracellular domain may also play a role. We have previously shown that the C-terminus of the extracellular loop 2 of CB1 is important in binding some compounds; receptors with mutations in this region (F268W, P269A, H270A, and I271A) bound some agonists with severely reduced affinity relative to the wild-type receptor. In the present work, we examine the impact of these mutations on binding a chemically diverse set of ligands. The receptors, F268W and I271A, exhibited a greater sensitivity to binding the inverse agonists/antagonists SLV319, AVE1625, NESS0327 relative to P269A and H270A, suggesting that the Pro and His are not involved in binding those compounds. In contrast, binding of the agonists, BAY593074 and WIN55212-2, was diminished in all four receptors, suggesting the conformational unit contributed by all four residues is important. A more marked loss in binding was observed for agonists of the nonclassical (CP55940) and classical (HU-210, JWH061, JWH179) cannabinoid classes and for a silent antagonist derivative (O-2050), pointing to the critical nature of this region for binding both the bicyclic/tricyclic core and the alkyl chain of these derivatives.
2.Cannabinoid receptor antagonists: pharmacological opportunities, clinical experience, and translational prognosis.
Janero DR;Makriyannis A Expert Opin Emerg Drugs. 2009 Mar;14(1):43-65. doi: 10.1517/14728210902736568 .
The endogenous cannabinoid (CB) (endocannabinoid) signaling system is involved in a variety of (patho)physiological processes, primarily by virtue of natural, arachidonic acid-derived lipids (endocannabinoids) that activate G protein-coupled CB1 and CB2 receptors. A hyperactive endocannabinoid system appears to contribute to the etiology of several disease states that constitute significant global threats to human health. Consequently, mounting interest surrounds the design and profiling of receptor-targeted CB antagonists as pharmacotherapeutics that attenuate endocannabinoid transmission for salutary gain. Experimental and clinical evidence supports the therapeutic potential of CB1 receptor antagonists to treat overweight/obesity, obesity-related cardiometabolic disorders, and substance abuse. Laboratory data suggest that CB2 receptor antagonists might be effective immunomodulatory and, perhaps, anti-inflammatory drugs. One CB1 receptor antagonist/inverse agonist, rimonabant, has emerged as the first-in-class drug approved outside the United States for weight control. Select follow-on agents (taranabant, otenabant, surinabant, rosonabant, SLV-319, AVE1625, V24343) have also been studied in the clinic.
3.Inhibition of THC-induced effects on the central nervous system and heart rate by a novel CB1 receptor antagonist AVE1625.
Zuurman L;Roy C;Schoemaker RC;Amatsaleh A;Guimaeres L;Pinquier JL;Cohen AF;van Gerven JM J Psychopharmacol. 2010 Mar;24(3):363-71. doi: 10.1177/0269881108096509. Epub 2008 Sep 18.
CB1 antagonists such as AVE1625 are potentially useful in the treatment of obesity, smoking cessation and cognitive impairment. Proof of pharmacological action of AVE1625 in the brain can be given by antagonising the effects of delta-9-tetrahydrocannabinol (THC), a CB1/CB2 agonist. Inhibition of THC-induced effects by AVE1625 was observed on Visual Analogue Scales 'alertness', 'feeling high', 'external perception', 'body sway' and 'heart rate'. Even the lowest dose of AVE1625 20 mg inhibited most of THC-induced effects. AVE1625 did not have any effect on psychological and behavioural parameters or heart rate by itself. After THC and AVE1625 administration, changes on electroencephalography were observed. This study shows a useful method for studying the effects of CB1 antagonists. AVE1625 penetrates the brain and antagonises THC-induced effects with doses at or above 20 mg.
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CAS 358970-97-5 Drinabant

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