Felbamate | W-554;ADD-03055;Taloxa.;Felbamyl;| 非氨酯 | NMDAR

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非尔氨酯 /Felbamate {[allProObj[0].p_purity_real_show]}

货号：A637947 同义名： 非氨酯 / W-554;ADD-03055

Felbamate is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA) .

Felbamate 化学结构
CAS号：25451-15-4

Felbamate 3D分子结构
CAS号：25451-15-4

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Felbamate 纯度/质量文件产品仅供科研

货号：A637947 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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NMDAR 亚型比较

产品名称	NMDA receptor ↓ ↑	其他靶点	纯度
Empirical Formula	✔		97%
Dizocilpine maleate	+++ NMDA receptor, Kd: 37.2 nM		99%+
Felbamate	+ NMDAR, IC50: 1.8 mM		98%
(-)-Dizocilpine maleate	++++ NMDA receptor, Ki: 30.5 nM		98%
Ifenprodil tartrate	+++ NMDA Receptor, IC50: 0.3 μM		98%
Spermidine	✔	Autophagy	98% GC
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Felbamate 生物活性

靶点

NMDA receptor

NMDAR, IC50:1.8 mM

描述

Felbamate, a novel anticonvulsant that binds to the glycine site of the N-methyl-D-aspartate receptor, has been shown to have neuroprotective properties in vitro and in vivo. In a rat pup model of hypoxia-ischemia, felbamate selectively reduced delayed death in hippocampal granule cells^[3]. Felbamate exhibits modest selectivity for NMDA (N-methyl-D-asparate) receptors composed of NR1a/NR2B subunits. Felbamate produced a rapid, concentration-dependent block of currents evoked by 50 microM NMDA and 10 microM glycine in human embryonic kidney 293 cells expressing the rat NR1a subunit, and either the NR2A, NR2B or NR2C subunits; the IC50 values for block were 2.6, 0.52 and 2.4 mM, respectively (holding potential, - 60 mV)^[4]. Felbamate decreased the magnitude of glycine (100 microM)-enhanced NMDA (100 microM)-induced intracellular calcium ([Ca2+]i) transients in mouse cerebellar granule cells which had been loaded with the Ca(2+)-sensitive fluorescent probe indo-1 acetoxymethyl ester (indo-1/AM)^[5]. Felbamate has antidepressant-like actions in mice involving the hippocampal BDNF (brain-derived neurotrophic factor) system^[6].

Felbamate 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
NCT00404248	Brain and Central Nervous Syst... 展开 >>em Tumors 收起 <<	Phase 1 Phase 2	Completed	-	United States, Alabama ... 展开 >> UAB Comprehensive Cancer Center Birmingham, Alabama, United States, 35294-3410 United States, Florida H. Lee Moffitt Cancer Center and Research Institute at University of South Florida Tampa, Florida, United States, 33612-9497 United States, Georgia Winship Cancer Institute of Emory University Atlanta, Georgia, United States, 30322 United States, Maryland Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Baltimore, Maryland, United States, 21231 United States, Massachusetts Massachusetts General Hospital Boston, Massachusetts, United States, 02114 United States, Michigan Josephine Ford Cancer Center at Henry Ford Hospital Detroit, Michigan, United States, 48202 United States, North Carolina Wake Forest University Comprehensive Cancer Center Winston-Salem, North Carolina, United States, 27157-1096 United States, Ohio Cleveland Clinic Taussig Cancer Center Cleveland, Ohio, United States, 44195 United States, Pennsylvania Abramson Cancer Center of the University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104-4283 收起 <<
NCT00404248	-		Completed	-	-
NCT01390909	-		Completed	-	-

Felbamate 参考文献

[1]Kuo CC, Lin BJ, et al. Use-dependent inhibition of the N-methyl-D-aspartate currents by felbamate: a gating modifier with selective binding to the desensitized channels. Mol Pharmacol. 2004 Feb;65(2):370-80.

[2]Subramaniam S, Rho JM, et al. Felbamate block of the N-methyl-D-aspartate receptor. J Pharmacol Exp Ther. 1995 May;273(2):878-86.

[3]Wasterlain CG, Adams LM, Wichmann JK, Sofia RD. Felbamate protects CA1 neurons from apoptosis in a gerbil model of global ischemia. Stroke. 1996 Jul;27(7):1236-40

[4]Harty TP, Rogawski MA. Felbamate block of recombinant N-methyl-D-aspartate receptors: selectivity for the NR2B subunit. Epilepsy Res. 2000 Mar;39(1):47-55

[5]White HS, Harmsworth WL, Sofia RD, Wolf HH. Felbamate modulates the strychnine-insensitive glycine receptor. Epilepsy Res. 1995 Jan;20(1):41-8

[6]Li X, Wang H, Chen Q, Li Z, Liu C, Yin S, You Z. Felbamate produces antidepressant-like actions in the chronic unpredictable mild stress and chronic social defeat stress models of depression. Fundam Clin Pharmacol. 2019 Dec;33(6):621-633

Felbamate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

4.20mL

0.84mL

0.42mL

20.99mL

4.20mL

2.10mL

41.97mL

8.39mL

4.20mL

Felbamate 技术信息

CAS号	25451-15-4
分子式	C₁₁H₁₄N₂O₄
分子量	238.24

别名	非氨酯 ;W-554;ADD-03055;Taloxa.;Felbamyl;brand name: Felbatol
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 105 mg/mL(440.73 mM)，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

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

NCT00404248	Brain and Central Nervous Syst... 展开 >>em Tumors 收起 <<	Phase 1 Phase 2	Completed	-	United States, Alabama ... 展开 >> UAB Comprehensive Cancer Center Birmingham, Alabama, United States, 35294-3410 United States, Florida H. Lee Moffitt Cancer Center and Research Institute at University of South Florida Tampa, Florida, United States, 33612-9497 United States, Georgia Winship Cancer Institute of Emory University Atlanta, Georgia, United States, 30322 United States, Maryland Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Baltimore, Maryland, United States, 21231 United States, Massachusetts Massachusetts General Hospital Boston, Massachusetts, United States, 02114 United States, Michigan Josephine Ford Cancer Center at Henry Ford Hospital Detroit, Michigan, United States, 48202 United States, North Carolina Wake Forest University Comprehensive Cancer Center Winston-Salem, North Carolina, United States, 27157-1096 United States, Ohio Cleveland Clinic Taussig Cancer Center Cleveland, Ohio, United States, 44195 United States, Pennsylvania Abramson Cancer Center of the University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104-4283 收起 <<
NCT00404248	-		Completed	-	-
NCT01390909	-		Completed	-	-
NCT00552526	Epilepsy Ment... 展开 >>al Retardation 收起 <<	Phase 4	Unknown	December 2013	Norway ... 展开 >> SSE, Nevrological dep. , Rikshospitalet University hospital Oslo, Norway 收起 <<
NCT00034229	Bipolar Disorder	Phase 2	Completed	-	United States, Maryland ... 展开 >> National Institute of Mental Health (NIMH) Bethesda, Maryland, United States, 20892 收起 <<
NCT01390909	-		Completed	-	-

非尔氨酯 /Felbamate {[allProObj[0].p_purity_real_show]}

Felbamate 纯度/质量文件产品仅供科研

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Felbamate 质控信息

Felbamate 生物活性

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Felbamate 参考文献

Felbamate 实验方案

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非尔氨酯 /Felbamate {[allProObj[0].p_purity_real_show]}

Felbamate 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Felbamate 质控信息

Felbamate 生物活性

Felbamate 临床研究

Felbamate 参考文献

Felbamate 实验方案

Felbamate 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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