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Submit ReviewFenobam
说明： Potent and selective mGlu5 negative allosteric modulator (NAM)
化学名： N-(3-Chlorophenyl)-N'-(4,5-dihydro-1-methyl-4-oxo-1H-imidazol-2-yl)urea
纯度： ≥99% (HPLC)
生物活性 for Fenobam
Fenobam is a potent and selective non-competitive mGlu5 negative allosteric modulator (NAM) that also displays inverse agonist properties; blocks mGlu5 constitutive activity in vitro (IC50 = 87 nM). Acts at an allosteric modulatory site shared with MPEP and binds the mGlu5 receptor with Kd values of 54 and 31 nM for rat and human receptors respectively. Displays anxiolytic activity following oral administration in vivo; also exhibits analgesic properties.
化合物库 for Fenobam
Fenobam is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for Fenobam
| 分子量 | 266.69 |
| 公式 | C11H11N4O2Cl |
| 储存 | Store at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 57653-26-6 |
| PubChem ID | 162834 |
| InChI Key | DWPQODZAOSWNHB-UHFFFAOYSA-N |
| Smiles | CN1CC(=O)N=C1NC(=O)NC1=CC(Cl)=CC=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Fenobam
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 26.67 | 100 |
制备储备液 for Fenobam
以下数据基于产品分子量 266.69。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.75 mL | 18.75 mL | 37.5 mL |
| 5 mM | 0.75 mL | 3.75 mL | 7.5 mL |
| 10 mM | 0.37 mL | 1.87 mL | 3.75 mL |
| 50 mM | 0.07 mL | 0.37 mL | 0.75 mL |
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产品说明书 for Fenobam
参考文献 for Fenobam
参考文献是支持产品生物活性的出版物。
Porter et al (2005) Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J.Pharmacol.Exp.Ther. 315 711 PMID: 16040814
Montana et al (2009) The metabotropic glutamate receptor subtype 5 antagonist fenobam is analgesic and has improved in vivo selectivity compared with the prototypical antagonist 2-methyl-6-(phenylethynyl)-pyridine. J.Pharmacol.Exp.Ther. 330 834 PMID: 19515968
Porter et al (2005) Description of a clinically validated anxiolytic with mGlu5 antagonist properties. Neuropharmacology 49 267
Kufahl et al (2013) Positive or negative allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) does not alter expression of behavioral sensitization to methamphetamine F1000Res. 1 10.12688/f1000resear PMID: 24358885
Liu et al (2018) Orthosteric and allosteric action of the C5a receptor antagonists Nature Structural & Molecular Biology 25 472 PMID: 29867214
If you know of a relevant reference for Fenobam, please let us know.
关键词: Fenobam, Fenobam supplier, Potent, selective, mGlu5, antagonist, mGluR5, antagonists, Group, I, Receptors, Glutamate, Metabotropic, (Metabotropic), 2386, Tocris Bioscience
1 篇 Fenobam 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Fenobam 的部分引用包括：
Crock et al (2012) Metabotropic glutamate receptor 5 (mGluR5) regulates bladder nociception. Mol Pain 8 20 PMID: 22449017
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Metabotropic Glutamate Receptors Scientific Review
Written by Francine Acher, this review discusses the pharmacology and therapeutic potential of mGlu receptors, and the compounds acting upon them; compounds available from Tocris are listed.
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