A non-competitive NMDA receptor antagonist that inhibits neuronal calcium channel currents; selective for NR2B subunit-containing receptors (IC50 = 1 µM)

Eliprodil – 50 mg

Brand:
Cayman
CAS:
119431-25-3
Storage:
-20
UN-No:
Non-Hazardous - /

N-Methyl-D-aspartate (NMDA) receptors are calcium permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. Eliprodil is a non-competitive NMDA receptor antagonist that inhibits neuronal calcium channel currents.{31071} It is selective for NR2B subunit-containing receptors (IC50 = 1 µM), displaying greater than 100-fold selectivity for NR2B over NR2A and NR2C subunits.{31074,31072} Eliprodil also avidly binds σ1 and σ2 sites (Kis = 0.013 and 0.63 µM, respectively).{31074} It is effective in vivo, blocking ischemia-induced neurodegeneration in the CA1 region of the hippocampus of gerbils subjected to bilateral carotid artery occlusion.{31071} Eliprodil can also have proarrhythmic actions in hearts under normal conditions.{31073}  

 

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Description

A non-competitive NMDA receptor antagonist that inhibits neuronal calcium channel currents; selective for NR2B subunit-containing receptors (IC50 = 1 µM), displaying greater than 100-fold selectivity for NR2B over NR2A and NR2C subunits

Formal name: α-​(4-​chlorophenyl)​-​4-​[(4-​fluorophenyl)​methyl]​-1-​piperidineethanol

Synonyms:  SL 820715

Molecular weight: 347.9

CAS: 119431-25-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Cardiovascular System|Cardiovascular Diseases|Stroke||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Neuroscience|Neurodegenerative Disorders

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