Eliprodil

Eliprodil is a non-competitive NMDA receptor antagonist that inhibits neuronal calcium channel currents.¹ It is selective for NR2B subunit-containing receptors (IC₅₀ = 1 µM), displaying greater than 100-fold selectivity for NR2B over NR2A and NR2C subunits.^2,3 Eliprodil also avidly binds σ₁ and σ₂ sites (K_is = 0.013 and 0.63 µM, respectively).² It is effective in vivo, blocking ischemia-induced neurodegeneration in the CA1 region of the hippocampus of gerbils subjected to bilateral carotid artery occlusion.¹ Eliprodil can also have proarrhythmic actions in hearts under normal conditions.⁴

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1. Bath, C.P., Farrell, L.N., Gilmore, J., et al. The effects of ifenprodil and eliprodil on voltage-dependent Ca²⁺ channels and in gerbil global cerebral ischaemia. Eur. J. Pharmacol. 299(1-3), 103-112 (1996).

2. Whittemore, E.R., Ilyin, V.I., and Woodward, R.M. Antagonism of N-methyl-D-aspartate receptors by σ site ligands: Potency, subtype-selectivity and mechanisms of inhibition. J. Pharmacol. Exp. Ther. 282(1), 326-338 (1997).

3. Grimwood, S., Richards, P., Murray, F., et al. 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. Neurochem. 75(6), 2455-2463 (2000).

4. Lengyel, C., Dézsi, L., Biliczki, P., et al. Effect of a neuroprotective drug, eliprodil on cardiac repolarisation: Importance of the decreased repolarisation reserve in the development of proarrhythmic risk. Brit. J. Pharmacol. 143(1), 152-158 (2004).