产品说明书

Fenobam

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Chemical Structure| 57653-26-6 同义名 : -
CAS号 : 57653-26-6
货号 : A529486
分子式 : C11H11ClN4O2
纯度 : 99%+
分子量 : 266.684
MDL号 : MFCD00868019
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(393.72 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Fenobam is a selective, orally active antagonist of mGluR5 with an IC50 of 84 nM and the ability to cross the blood-brain barrier. The Kd values of Fenobam for rat and human recombinant mGlu5 receptors are 54 nM and 31 nM, respectively. Fenobam exhibits anti-anxiety properties, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. It is used in research related to neurological disorders, cancer, and drug addiction[1][2][3]. At a concentration of 300 μM, a 72-hour treatment with Fenobam significantly inhibits the proliferation of LM7 cells and induces apoptosis[2].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01981395 Hyperalgesia ... 展开 >>Allodynia 收起 << Phase 1 Completed - United States, Missouri ... 展开 >> Washington University School of Medicine St. Louis, Missouri, United States, 63110 收起 <<
NCT01806415 Healthy Phase 1 Completed - United States, Missouri ... 展开 >> Washington University School Of Medicine St. Louis, Missouri, United States, 63110 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.75mL

0.75mL

0.37mL

18.75mL

3.75mL

1.87mL

37.50mL

7.50mL

3.75mL

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]Liao S, et al. Osteosarcoma cell proliferation and survival requires mGluR5 receptor activity and is blocked by Riluzole. PLoS One. 2017 Feb 23;12(2):e0171256.

[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.