| Identification | Back Directory | [Name]
Drinabant | [CAS]
358970-97-5 | [Synonyms]
AVE-1625
drinabant
N-[1-[Bis(4-chlorophenyl)methyl]azetidin-3-yl]-N-(3,5-difluorophenyl)methanesulfonamide
Methanesulfonamide, N-[1-[bis(4-chlorophenyl)methyl]-3-azetidinyl]-N-(3,5-difluorophenyl)- | [Molecular Formula]
C23H20Cl2F2N2O2S | [MDL Number]
MFCD10567084 | [MOL File]
358970-97-5.mol | [Molecular Weight]
497.38 |
| Chemical Properties | Back Directory | [Boiling point ]
581.7±60.0 °C(Predicted) | [density ]
1.458 | [storage temp. ]
Store at -20°C | [solubility ]
≤0.15mg/ml in ethanol;15mg/ml in DMSO;15mg/ml in dimethyl formamide | [form ]
crystalline solid | [pka]
5.44±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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. Signaling through the CB1 receptor is implicated in attentional and working memory deficits as well as obesity. AVE-1625 is a highly potent, selective antagonist for the CB1 receptor with Ki values of 0.16-0.44 nM. At 1-3 mg/kg, AVE-1625 significantly improves the performance of rodents in working memory tasks. 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. | [Uses]
AVE-1625 is a selective antagonist for the CB1 receptor. | [storage]
Store at -20°C | [References]
[1] borowsky b, stevens r, mark b, et al. ave1625, a cannabinoid cbi antagonist, as a co-treatment for schizophrenia: improvement in cognitive function and reduction of antipsychotic-side effects in animal models[c]//neuropsychopharmacology. macmillan building, 4 crinan st, london n1 9xw, england: nature publishing group, 2005, 30: s116-s117.
[2] herkenham m, lynn a b, little m d, et al. cannabinoid receptor localization in brain[j]. proceedings of the national academy of sciences, 1990, 87(5): 1932-1936.
[3] herling a w, gossel m, haschke g, et al. cb1 receptor antagonist ave1625 affects primarily metabolic parameters independently of reduced food intake in wistar rats[j]. american journal of physiology-endocrinology and metabolism, 2007, 293(3): e826-e832. |
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