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알파-(4-클로로페닐)-4-[(4-플루오로페닐)메틸]-1-피페리딘에탄올 C화학적 특성, 용도, 생산
개요
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. It is selective for NR2B subunit-containing receptors (IC50 = 1 μM), displaying greater than 100-fold selectivity for NR2B over NR2A and NR2C subunits. Eliprodil also avidly binds σ1 and σ2 sites (Kis = 0.013 and 0.63 μM, respectively). It is effective in vivo, blocking ischemia-induced neurodegeneration in the CA1 region of the hippocampus of gerbils subjected to bilateral carotid artery occlusion. Eliprodil can also have proarrhythmic actions in hearts under normal conditions.
용도
Eliprodil is a noncardiac drug with neuroprotective properties. It is also a N-Methyl-D-aspartate receptor (NMDAR) antagonist.
생물학적 활성
Non-competitive NMDA receptor antagonist that acts at the polyamine modulatory site. Selective for NR2B- over NR2A- and NR2C-containing receptors (IC 50 values are 1, > 100 and > 100 μ M respectively). Also σ 1 ligand (K i = 0.013 μ M). Antagonizes neuronal voltage-gated Ca 2+ channels and selectively inhibits the rapid component of the delayed rectifier K + current (I Kr ). Neuroprotective.
알파-(4-클로로페닐)-4-[(4-플루오로페닐)메틸]-1-피페리딘에탄올 준비 용품 및 원자재
![알파-(4-클로로페닐)-4-[(4-플루오로페닐)메틸]-1-피페리딘에탄올](CAS/GIF/119431-25-3.gif)
