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EliprodilCat. No. 2195 |
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Chemical Name: α-(4-Chlorophenyl)-4-[(4-fluorophenyl)methyl]-1-piperidineethanol |
Biological Activity
Non-competitive NMDA receptor antagonist that acts at the polyamine modulatory site. Selective for NR2B- over NR2A- and NR2C-containing receptors (IC50 values are 1, > 100 and > 100 μM respectively). Also σ1 ligand (Ki = 0.013 μM). Antagonizes neuronal voltage-gated Ca2+ channels and selectively inhibits the rapid component of the delayed rectifier K+ current (IKr). Neuroprotective.Certificate of Analysis / Safety Data Sheet
References
Bath et al (1996) The effects of ifenprodil and eliprodil on voltage-dependent Ca2+ channels and in gerbil global cerebral ischaemia. Eur.J.Pharmacol. 299 103. PMID: 8901012.
Whittemore et al (1997) Antagonism of N-methyl-D-aspartate receptors by σ site ligands: potency, subtype-selectivity and mechanisms of inhibition. J.Pharmacol.Exp.Ther. 282 326. PMID: 9223571.
Lengyel et al (2004) Effect of a neuroprotective drug, eliprodil on cardiac repolarisation: importance of the decreased repolarisation reserve in the development of proarrhythmic risk. Br.J.Pharmacol. 143 152. PMID: 15302678.
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Keywords: Eliprodil, supplier, σ, sigma, ligands, σ1, sigma1, σ2, sigma2, polyamine, site, NMDA, antagonists, Ca2+, channel, blockers, Neuroprotective, Non-competitive, NR2B-selective, Receptors, Glutamate, N-Methyl-D-Aspartate, iGluR, Ionotropic
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