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Fenobam(hydrate)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Fenobam(hydrate)图片
CAS NO:63540-28-3
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
A noncompetitive antagonist and inverse agonist of mGluR5
Cas No.63540-28-3
Canonical SMILESClC1=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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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)