生物活性 | |||
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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 | |||||
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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 | |||
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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 |
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