Chemical Name:a-(4-Chlorophenyl)-4-[(4-fluorophenyl)methyl]-1-piperid
ineethanol
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).
Antagonises neuronal voltage-gated Ca2+ channels and selectively
inhibits the rapid component of the delayed rectifier K+ current (IKr).
Neuroprotective.
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References:
Bathet al
(1996) The effects of ifenprodil and eliprodil on voltage-dependent Ca2+
channels and in gerbil global cerebral ischaemia. Eur.J.Pharmacol. 299
103. Whittemoreet 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. 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.
Displays 26-fold and > 440-fold selectivity over kainate and NMDA receptors respectively. Neuro-protective; delays neuronal death in a global ischaemia model and cerebral infarction in a focal ischaemia model.
