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CAS No.: 119431-25-3

Eliprodil/依利罗地 Catalog No. CSN10256

Synonyms: SL-820715;SL-82,0715

Eliprodil can antogonize GluN2B-selective NMDA in a non-competitive manner with IC50 value of 1 μM. It is also a σ1 ligand with Ki value of 0.013 μM.

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实验方案

技术信息

生物活性

描述Eliprodil is a non-competitive NR2B-NMDA (NR2B-selective N-methyl-D-aspartate) receptor antagonist(IC50=10 microM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM)^[3]. Eliprodil significantly decreased the amplitude of rapid component of the delayed rectifier potassium current (I(Kr)), but slow component (I(Ks)), transient outward current (I(to)) and I(K1) were not considerably affected by the drug when measured in dog ventricular myocytes by applying the whole-cell configuration of the patch-clamp technique. Eliprodil, under normal conditions, moderately lengthens cardiac repolarisation by inhibition of I(Kr)^[4]. Eliprodil administered intraperitoneally at 10 mg/kg completely prevented the loss of ChAT (choline acetyltransferase) and the loss of cells in the GCL(ganglion cell layer) ^[5]. A low dose of eliprodil (5 mg/kg) weakly stimulated locomotion in naive animals, whilst higher doses depressed rearing (20-40 mg/kg) and grooming (40 mg/kg), consistent with a sedative action^[6]. The administration of a neuroprotective drug (eliprodil) or a thrombolytic agent (rt-PA) similarly reduce the volume of brain damage and the neurological deficit in a rat embolic stroke model^[7].
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
NCT00001929	Movement Disorders ... more >> Parkinson Disease Collapse <<	Phase 2	Completed	-	United States, Maryland ... more >> National Institute of Neurological Disorders and Stroke (NINDS) Bethesda, Maryland, United States, 20892 Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8748 mL
- 14.3738 mL
- 28.7477 mL
- 5 mM
- 0.5750 mL
- 2.8748 mL
- 5.7495 mL
- 10 mM
- 0.2875 mL
- 1.4374 mL
- 2.8748 mL

技术信息

CAS号

119431-25-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H23ClFNO

运输

蓝冰

分子量

347.85

别名

SL-820715;SL-82,0715

溶解度

DMSO	50.0 mg/mL (143.7 mM) warming
Water	insoluble

动物实验配方

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Eliprodil/依利罗地 Catalog No. CSN10256

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