| 产品描述： | Fenobam is a selective, orally active, and brain-penetrant mGluR5 antagonist acting at an allosteric modulatory site (Kds of 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 |
| 靶点： |
rat mGluR5:54 nM (Kd);human mGluR5:31 nM (Kd) |
| 体内研究： |
Fenobam sulfate (30-60 mg/kg; po) 显著抑制自我给药行为。 Animal Model: Male Long-Evans rats (250-300 g) Dosage: 30-60 mg/kg Administration: P.o. Result: Inhibited self-administration |
| 参考文献： |
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; 3. Keck TM, et al. Fenobam sulfate inhibits cocaine-taking and cocaine-seeking behavior in rats: implications for addiction treatment in humans. Psychopharmacology (Berl). 2013;229(2):253-265. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.75 ml |
18.749 ml |
37.498 ml |
| 5 mM |
0.75 ml |
3.75 ml |
7.5 ml |
| 10 mM |
0.375 ml |
1.875 ml |
3.75 ml |
| 50 mM |
0.075 ml |
0.375 ml |
0.75 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京