Eliprodil

• CAT Number: I000706
• CAS Number: 119431-25-3
• Molecular Formula: C20H23ClFNO
• Molecular Weight: 347.9
• Purity: ≥95%
• Synonyms: (R)-1-(4-chlorophenyl)-2-(4-(4-fluorobenzyl)piperidin-1-yl)ethanol
• Target: NMDA Receptor
• Solubility: 10 mM in DMSO
• Storage: Desiccate at +4C
• InChIKey: GGUSQTSTQSHJAH-UHFFFAOYSA-N

Eliprodil (CAT: I000706) is a non-competitive antagonist of the NR2B subunit of the N-methyl-D-aspartate (NMDA) receptor. It exhibits an inhibitory effect on NR2B-containing receptors with an IC50 value of approximately 1 μM. Eliprodil is less potent in inhibiting NR2A- and NR2C-containing receptors. The NMDA receptor is involved in various physiological and pathological processes in the central nervous system, and the selective blockade of specific receptor subunits like NR2B has been investigated as a potential therapeutic strategy for conditions such as neurodegenerative diseases and pain management.

Reference

1:Effect of a neuroprotective drug, eliprodil on cardiac repolarisation: importance of the decreased repolarisation reserve in the development of proarrhythmic risk. Lengyel C, Dézsi L, Biliczki P, Horváth C, Virág L, Iost N, Németh M, Tálosi L, Papp JG, Varró A.Br J Pharmacol. 2004 Sep;143(1):152-8. Epub 2004 Aug 9. PMID: 15302678 Free PMC Article2:Administration of eliprodil during ethanol withdrawal in the neonatal rat attenuates ethanol-induced learning deficits. Thomas JD, Garcia GG, Dominguez HD, Riley EP.Psychopharmacology (Berl). 2004 Sep;175(2):189-95. Epub 2004 Apr 3. PMID: 15064913 3:Synthesis and resolution of racemic eliprodil and evaluation of the enantiomers of eliprodil as NMDA receptor antagonists. Pabel J, Höfner G, Wanner KT.Bioorg Med Chem Lett. 2000 Jun 19;10(12):1377-80. PMID: 10890168 4:Neuroprotective effects of eliprodil in retinal excitotoxicity and ischemia. Kapin MA, Doshi R, Scatton B, DeSantis LM, Chandler ML.Invest Ophthalmol Vis Sci. 1999 May;40(6):1177-82. PMID: 10235551 5:Protection by eliprodil against excitotoxicity in cultured rat retinal ganglion cells. Pang IH, Wexler EM, Nawy S, DeSantis L, Kapin MA.Invest Ophthalmol Vis Sci. 1999 May;40(6):1170-6. PMID: 10235550 6:Anticonvulsant effects of eliprodil alone or combined with the glycineB receptor antagonist L-701,324 or the competitive NMDA antagonist CGP 40116 in the amygdala kindling model in rats. Wlaź P, Ebert U, Löscher W.Neuropharmacology. 1999 Feb;38(2):243-51. PMID: 10218865 7:Eliprodil stimulates CNS myelination: new prospects for multiple sclerosis? Demerens C, Stankoff B, Zalc B, Lubetzki C.Neurology. 1999 Jan 15;52(2):346-50. PMID: 9932955 8:Place conditioning of mice with the NMDA receptor antagonists, eliprodil and dizocilpine. Sukhotina I, Dravolina O, Bespalov A.Eur J Pharmacol. 1998 Dec 4;362(2-3):103-10. PMID: 9874159 9:The effect of eliprodil on the evolution of a focal cerebral ischaemia in vivo. Ibarrola D, Seegers H, Jaillard A, Hommel M, Décorps M, Massarelli R.Eur J Pharmacol. 1998 Jul 3;352(1):29-35. PMID: 9718264 10:Neuroprotective effect of eliprodil: attenuation of a conditioned freezing deficit induced by traumatic injury of the right parietal cortex in the rat. Hogg S, Perron C, Barnéoud P, Sanger DJ, Moser PC.J Neurotrauma. 1998 Jul;15(7):545-53. PMID: 9674557