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| | Eliprodil Basic information |
| Product Name: | Eliprodil | | Synonyms: | SL 820715;ALPHA-(4-CHLOROPHENYL)-4-[(4-FLUOROPHENYL)METHYL]-1-PIPERIDINEETHANOL;ELIPRODIL;α-(4-chlorophenyl)-4-[(4-fluorophenyl)methyl]-1-piperidineethanol;SL 820715, α-(4-Chlorophenyl)-4-[(4-fluorophenyl)methyl]-1-piperidineethanol;(+-)-alpha-(p-Chlorophenyl)-4-(p-fluorobenzyl)-1-piperidineethanol;1-(4-broMophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethanol;1-Piperidineethanol, α-(4-chlorophenyl)-4-[(4-fluorophenyl)methyl]- | | CAS: | 119431-25-3 | | MF: | C20H23ClFNO | | MW: | 347.85 | | EINECS: | | | Product Categories: | Inhibitors;Glutamate receptor;Neuroprotective agent. | | Mol File: | 119431-25-3.mol |  |
| | Eliprodil Chemical Properties |
| Boiling point | 474.1±35.0 °C(Predicted) | | density | 1.205±0.06 g/cm3(Predicted) | | storage temp. | Sealed in dry,2-8°C | | solubility | DMSO: ~17 mg/mL | | form | solid | | pka | 13.99±0.20(Predicted) | | color | white |
| Hazard Codes | N | | Risk Statements | 50/53 | | Safety Statements | 60-61 | | RIDADR | UN 3077 9/PG 3 | | WGK Germany | 3 |
| | Eliprodil Usage And Synthesis |
| Description | 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. | | Uses | Eliprodil is a noncardiac drug with neuroprotective properties. It is also a N-Methyl-D-aspartate receptor (NMDAR) antagonist. | | Definition | ChEBI: Eliprodil is a racemate comprising equimolar amounts of (R)- and (S)-eliprodil. It is a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist and an anti-ischaemic agent that exhibits neuroprotective properties. It has a role as a geroprotector, a NMDA receptor antagonist, a neuroprotective agent and a calcium channel blocker. It contains a (R)-eliprodil and a (S)-eliprodil. | | Biological Activity | Eliprodil (SL-820715) is a non-competitive, NR2B-selective NMDA antagonist with IC50 of 1 μM. Its IC50 is greater than 100 μM for receptors containing NR2A and NR2C. | | Biological Activity | 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. | | storage | +4°C (desiccate) |
| | Eliprodil Preparation Products And Raw materials |
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