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Fenobam 是一种选择性、口服活性、能穿透血脑屏障的 mGluR5 拮抗剂,作用于别构调节位点(在大鼠和人重组 mGlu5 受体上的 Kd 值分别为 54 nM 和 31 nM)。Fenobam 具有反向激动剂活性,IC50 为 84 nM,阻断 mGlu5 受体活性,具有抗焦虑作用。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Fenobam 化学结构 CAS号:57653-26-6
Fenobam 化学结构
CAS号:57653-26-6
Fenobam 3D分子结构
CAS号:57653-26-6
Fenobam 化学结构 CAS号:57653-26-6
Fenobam 3D分子结构 CAS号:57653-26-6
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Fenobam 纯度/质量文件 产品仅供科研

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Fenobam 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].

Fenobam 动物研究

Animal study Administered orally at doses of 30-60 mg/kg three times a week, Fenobam significantly suppresses self-administration behavior in rats[3].

Fenobam 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 <<

Fenobam 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.

Fenobam 实验方案

计算器
存储液制备 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

Fenobam 技术信息

CAS号57653-26-6
分子式C11H11ClN4O2
分子量 266.684
别名
运输蓝冰
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
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