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 (IC
50 = 1 μM), displaying greater than 100-
fold selectivity for NR2B over NR2A and NR2C subunits. Eliprodil also avidly binds σ
1 and σ
2 sites (K
is = 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.
References
[1] CATHERINE P. BATH. The effects of ifenprodil and eliprodil on voltage-dependent Ca2+ channels and in gerbil global cerebral ischaemia[J]. European journal of pharmacology, 1996, 299 1: Pages 103-112. DOI:
10.1016/0014-2999(95)00846-2[2] E R WHITTEMORE R M W V I Ilyin. Antagonism of N-methyl-D-aspartate receptors by sigma site ligands: potency, subtype-selectivity and mechanisms of inhibition.[J]. Journal of Pharmacology and Experimental Therapeutics, 1997, 282 1: 326-338.
[3] SARAH GRIMWOOD. Characterisation of N-Methyl-D-Aspartate Receptor-Specific [3H]Ifenprodil Binding to Recombinant Human NR1a/NR2B Receptors Compared with Native Receptors in Rodent Brain Membranes[J]. Journal of Neurochemistry, 2008, 75 6: 2455-2463. DOI:
10.1046/j.1471-4159.2000.0752455.x[4] CSABA LENGYEL. Effect of a neuroprotective drug, eliprodil on cardiac repolarisation: importance of the decreased repolarisation reserve in the development of proarrhythmic risk[J]. British Journal of Pharmacology, 2009, 143 1: 152-158. DOI:
10.1038/sj.bjp.0705901
