Eliprodil
Chemical Name: α-(4-Chlorophenyl)-4-[(4-fluorophenyl)methyl]-1-piperidineethanol
Purity: ≥98%
Biological Activity
Eliprodil is a non-competitive NMDA receptor antagonist that acts at the polyamine modulatory site. Selective for GluN2B (formally NR2B)- over GluN2A (NR2A)- and GluN2C (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.Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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The effects of ifenprodil and eliprodil on voltage-dependent Ca2+ channels and in gerbil global cerebral ischaemia.
Bath et al.
Eur.J.Pharmacol., 1996;299:103 -
Antagonism of N-MthD.-aspartate receptors by σ site ligands: potency, subtype-selectivity and mechanisms of inhibition.
Whittemore et al.
J.Pharmacol.Exp.Ther., 1997;282:326 -
Effect of a neuroprotective drug, eliprodil on cardiac repolarisation: importance of the decreased repolarisation reserve in the development of proarrhythmic risk.
Lengyel et al.
Br.J.Pharmacol., 2004;143:152
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Citations for Eliprodil
The citations listed below are publications that use Tocris products. Selected citations for Eliprodil include:
2 Citations: Showing 1 - 2
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σ1 receptor ligands control a switch between passive and active threat responses.
Authors: Rennekamp Et al.
Nat Chem Biol 2016;12:552
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Molecular pharmacology of human NMDA receptors.
Authors: Hedegaard Et al.
Neurochem Int 2012;61:601
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We studied the histological assessment of the volume of the traumatic brain lesion to estimate the extent of the structural damage. In the study, we have used this approach to evaluate the efficacity and the window of therapeutic opportunity of Eliprodil.
