非诺班

非诺班用途

Fenobam 是一种选择性、口服活性、非竞争性的 mGluR5 拮抗剂,其作用于变构调节位点 (在大鼠和人重组 mGlu5 受体上的 Kd 值分别 54 nM 和 31 nM)。Fenobam 具有反向激动剂活性,其阻断 mGlu5 受体活性,IC50为 84 nM。 Fenobam 具有抗焦虑活性。

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非诺班名称

[ CAS 号 ]:
57653-26-6

[ 中文名 ]:
非诺班

[ 英文名 ]:
Fenobam

[中文别名 ]:

苯脲咪唑酮

[英文别名 ]:

Mcn-3377
[3H]-Fenobam

非诺班生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 谷氨酸受体

研究领域 >> 神经疾病

[ 靶点 ]

rat mGluR5:54 nM (Kd)

human mGluR5:31 nM (Kd)

[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;

非诺班物理化学性质

[ 密度 ]:
1.47 g/cm3

[ 分子式 ]:
C₁₁H₁₁ClN₄O₂

[ 分子量 ]:
266.68400

[ 精确质量 ]:
266.05700

[ PSA ]:
73.80000

[ LogP ]:
1.12690

[ 折射率 ]:
1.668

[ 储存条件 ]:
2-8°C

非诺班MSDS

详细MSDS(安全技术说明书)

非诺班安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300

[ 警示性声明 ]:
Missing Phrase - N15.00950417

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

非诺班文献

Pharmacophoric features of drugs with guanylurea moiety: an electronic structure analysis.

J. Mol. Model. 19(4) , 1865-74, (2013)

Several therapeutically important compounds contain guanylurea (GU) moiety. The appropriate tautomeric state of these species has not been explored, preliminary studies indicated that the traditional ...

Inhibition of Group I Metabotropic Glutamate Receptors Reverses Autistic-Like Phenotypes Caused by Deficiency of the Translation Repressor eIF4E Binding Protein 2.

J. Neurosci. 35 , 11125-32, (2015)

Exacerbated mRNA translation during brain development has been linked to autism spectrum disorders (ASDs). Deletion of the eukaryotic initiation factor 4E (eIF4E)-binding protein 2 gene (Eif4ebp2), en...

Insights into the interaction of negative allosteric modulators with the metabotropic glutamate receptor 5: discovery and computational modeling of a new series of ligands with nanomolar affinity.

Bioorg. Med. Chem. 23 , 3040-58, (2015)

Metabotropic glutamate receptor 5 (mGlu5) is a biological target implicated in major neurological and psychiatric disorders. In the present study, we have investigated structural determinants of the i...

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非诺班