CAS NO: | 63540-28-3 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
Cas No. | 63540-28-3 |
Canonical SMILES | ClC1=CC=CC(NC(NC(N(C)C2)=NC2=O)=O)=C1.O |
分子式 | C11H11ClN4O2.H2O |
分子量 | 284.7 |
溶解度 | DMSO: 100 mM |
储存条件 | Store at -20°C |
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 | Fenobam is a noncompetitive antagonist and inverse agonist of metabotropic glutamate receptor 5 (mGluR5) that binds to an allosteric site.1It inhibits intracellular calcium mobilization induced by the glutamate analog quisqualate in HEK293 cells expressing the human receptor (IC50= 58 nM) and inhibits basal activity of mGluR5 in a cell-based assay (IC50= 84 nM).1Fenobam (10 and 30 mg/kg) reduces stress-induced hyperthermia in mice and increases drinking time in the Vogel conflict test in rats when administered at a dose of 30 mg/kg, indicating anxiolytic-like activity. It induces analgesia in the formalin test in mice when administered at a dose of 30 mg/kg.2 1.Porter, R.H.P., Jaeschke, G., Spooren, W., et al.Fenobam: A clinically validated nonbenzodiazepine anxiolytic Is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activityJ. Pharmacol. Exp. Ther.315(2)711-721(2005) 2.Montana, M.C., Conrardy, B.A., Cavallone, L.F., et al.Metabotropic glutamate receptor 5 antagonism with fenobam: Examination of analgesic tolerance and side effect profile in miceAnesthesiology115(6)1239-1250(2011) |