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首页 / 抑制剂/激动剂 / 神经信号通路 /
NMDAR
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/ Eliprodil

依利罗地 /Eliprodil {[allProObj[0].p_purity_real_show]}

货号：A782266 同义名： SL-820715 Ambeed 开学季，买赠积分，赢豪礼

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.

Eliprodil 化学结构 CAS号：119431-25-3
Eliprodil 化学结构
CAS号：119431-25-3
Eliprodil 3D分子结构
CAS号：119431-25-3
Eliprodil 化学结构 CAS号：119431-25-3
Eliprodil 3D分子结构 CAS号：119431-25-3
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Eliprodil 纯度/质量文件 产品仅供科研

货号：A782266 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 NMDA receptor ↓ 其他靶点 纯度
Empirical Formula ✔ {[allProObj[0].p_purity_real_show]}
Dizocilpine maleate +++

NMDA receptor, Kd: 37.2 nM

 		{[allProObj[0].p_purity_real_show]}
Felbamate +

NMDAR, IC50: 1.8 mM

 		{[allProObj[0].p_purity_real_show]}
(-)-Dizocilpine maleate ++++

NMDA receptor, Ki: 30.5 nM

 		{[allProObj[0].p_purity_real_show]}
Ifenprodil tartrate +++

NMDA Receptor, IC50: 0.3 μM

 		{[allProObj[0].p_purity_real_show]}
Spermidine ✔ Autophagy {[allProObj[0].p_purity_real_show]}
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。
产品名称 AMPA receptor ↓ GluR ↓ mGluR5 ↓ NMDA receptor ↓ 其他靶点 纯度
Evans Blue ✔ {[allProObj[0].p_purity_real_show]}
IEM-1754 +

GluR3, IC50: 6 μM

GluR1, IC50: 6 μM

 		{[allProObj[0].p_purity_real_show]}
Latrepirdine 2HCl ✔ {[allProObj[0].p_purity_real_show]}
(-)-Huperzine A +++

AChE (G4 form), Ki: 7 nM

 		{[allProObj[0].p_purity_real_show]}
CTEP ++++

mGlu5, IC50: 2.2 nM

 		{[allProObj[0].p_purity_real_show]}
MPEP ++

mGluR5, IC50: 36 nM

 		{[allProObj[0].p_purity_real_show]}
Riluzole ✔ {[allProObj[0].p_purity_real_show]}
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。

Eliprodil 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].

Eliprodil 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 ... 展开 >> Parkinson Disease 收起 << Phase 2 Completed - United States, Maryland ... 展开 >> National Institute of Neurological Disorders and Stroke (NINDS) Bethesda, Maryland, United States, 20892 收起 <<

Eliprodil 参考文献

[1]Lengyel C, Dezsi L, et al. Effect of a neuroprotective drug, eliprodil on cardiac repolarisation: importance of the decreased repolarisation reserve in the development of proarrhythmic risk. Br J Pharmacol. 2004 Sep;143(1):152-8. Epub 2004 Aug 9.

[2]Bath CP, Farrell LN, et al. The effects of ifenprodil and eliprodil on voltage-dependent Ca2+ channels and in gerbil global cerebral ischaemia. Eur J Pharmacol. 1996 Mar 28;299(1-3):103-12.

[3]Bath CP, Farrell LN, Gilmore J, Ward MA, Hicks CA, O'Neill MJ, Bleakman D. The effects of ifenprodil and eliprodil on voltage-dependent Ca2+ channels and in gerbil global cerebral ischaemia. Eur J Pharmacol. 1996 Mar 28;299(1-3):103-12

[4]Lengyel C, Dézsi L, Biliczki P, Horváth C, Virág L, Iost N, Németh M, Tálosi L, Papp JG, Varró A. Effect of a neuroprotective drug, eliprodil on cardiac repolarisation: importance of the decreased repolarisation reserve in the development of proarrhythmic risk. Br J Pharmacol. 2004 Sep;143(1):152-8

[5]Kapin MA, Doshi R, Scatton B, DeSantis LM, Chandler ML. Neuroprotective effects of eliprodil in retinal excitotoxicity and ischemia. Invest Ophthalmol Vis Sci. 1999 May;40(6):1177-82

[6]Brooks S, Kaur S, Starr BS, Starr MS. Motor actions of eliprodil in the normal and monoamine-depleted mouse: a role in the treatment of Parkinson's disease? J Neural Transm (Vienna). 1996;103(6):737-48

[7]Lekieffre D, Benavides J, Scatton B, Nowicki JP. Neuroprotection afforded by a combination of eliprodil and a thrombolytic agent, rt-PA, in a rat thromboembolic stroke model. Brain Res. 1997 Nov 21;776(1-2):88-95

Eliprodil 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.87mL

0.57mL

0.29mL

14.37mL

2.87mL

1.44mL

28.75mL

5.75mL

2.87mL

Eliprodil 技术信息

CAS号119431-25-3
分子式C20H23ClFNO
分子量 347.854
别名 SL-820715
运输蓝冰
存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 15 mg/mL(43.12 mM)，配合低频超声助溶，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

Tags: Eliprodil | 119431-25-3 | SL-820715 | SL820715 | SL 820715 | iGluR Antagonist | Membrane Transporter/Ion Channel | Neuronal Signaling | iGluR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Eliprodil 纯度/质量文件 | Eliprodil 亚型比较 | Eliprodil 生物活性 | Eliprodil 临床数据 | Eliprodil 参考文献 | Eliprodil 实验方案 | Eliprodil 技术信息

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