Fenobam 是一种选择性、口服活性和脑渗透性 mGluR5 拮抗剂，作用于变构调节位点（大鼠和人重组 mGlu5 受体的 Kd 分别为 54 和 31 nM）。
| Cas No. | 57653-26-6 |
| 别名 | 非诺班 |
| 化学名 | 1-(3-chlorophenyl)-3-(1-methyl-4-oxo-4,5-dihydro-1H-imidazol-2-yl)urea |
| Canonical SMILES | ClC1=CC(NC(NC(N(C)C2)=NC2=O)=O)=CC=C1 |
| 分子式 | C11H11N4O2Cl |
| 分子量 | 266.69 |
| 溶解度 | <26.67mg/ml in DMSO |
| 储存条件 | Store at RT |
| 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 selective, orally active, and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively). Fenobam displays inverse agonist activity which blocks the mGlu5 receptor basal activity with an IC50 of 84 nM. Fenobam exerts anxiolytic activity[1][2]. References:
[1]. Porter RH, et al. Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J Pharmacol Exp Ther. 2005 Nov;315(2):711-21.
[2]. Laura F, et al. The Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Fenobam: Pharmacokinetics, Side Effects, and Analgesic Effects in Healthy Human Subjects.bioRxiv 391383; |
