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Eliprodil

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Chemical Structure| 119431-25-3 同义名 : SL-820715
CAS号 : 119431-25-3
货号 : A782266
分子式 : C20H23ClFNO
纯度 : 99%+
分子量 : 347.854
MDL号 : MFCD00866651
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：
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 ... 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 <<
实验方案
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
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