CAS NO: | 358970-97-5 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
Cas No. | 358970-97-5 |
别名 | 屈那班,Drinabant |
化学名 | N-[1-[bis(4-chlorophenyl)methyl]azetidin-3-yl]-N-(3,5-difluorophenyl)methanesulfonamide |
Canonical 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 |
分子式 | C23H20Cl2F2N2O2S |
分子量 | 497.4 |
溶解度 | ≤0.15mg/ml in ethanol;15mg/ml in DMSO;15mg/ml in dimethyl formamide |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | AVE-1625 is a highly potent, selective antagonist for the CB1 receptor [1]. The cannabinoid receptor type 1 (CB1) is a G protein-coupled receptor mainly expressed in the central and peripheral nervous system. The CB1 receptor is activated by the endocannabinoid neurotransmitters anandamide and 2-arachidonoylglycerol (2-AG). The CB1 receptor has been implicated in the maintenance of homeostasis in health and disease [2]. The CB1 receptor plays vital roles in modulating neurotransmitter release by preventing the development of excessive neuronal activity, reducing pain and other inflammatory symptoms [2]. AVE-1625 antagonized the CB1 receptor activity with the Ki values of 0.16-0.44 nM [1]. Treatment with AVE-1625 (1-3 mg/kg) significantly improved the performance of rodents in working memory tasks. At 30 mg/kg, AVE-1625 reduced caloric intake by more than 50% of controls and significantly increased lipolysis from fat tissues and reduced hepatic glycogen levels in rodents. In Wistar rats, postprandially administration of AVE1625 slightly increased the basal lipolysis in a dose-dependent manner. AVE1625 caused primary effects on metabolic blood and tissue parameters as well as metabolic rate [3]. As measured by indirect calorimetry, AVE1625 immediately increased the total energy expenditure and a transiently increased glucose oxidation [3]. References: |