The NMDA receptor antagonist eliprodil (SL 82.0715) blocks voltage-operated Ca2+ channels in rat cultured cortical neurons

Eur J Pharmacol. 1994 May 23;257(3):297-301. doi: 10.1016/0014-2999(94)90142-2.


The effect of the non-competitive NMDA receptor antagonist eliprodil on NMDA receptor- and voltage-operated Ca2+ currents was investigated in rat cultured cortical neurons by using the whole-cell patch clamp technique. With neurons voltage-clamped at -40 mV, eliprodil reduced in a concentration-dependent manner the inward current induced by N-methyl-D-aspartate (NMDA) (10 microM) in the presence of D-serine with an IC50 of 0.67 microM (Imax = 83%). Eliprodil also blocked the total inward Ba2+ current carried in part by L- and N-type Ca2+ channels with an IC50 of 1.48 microM (Imax = 87%). These results suggest that the neuroprotective properties of eliprodil could be due to its combined ability to antagonize the NMDA receptor- and voltage-operated Ca2+ channels.

MeSH terms

  • Animals
  • Calcium Channels / drug effects*
  • Cells, Cultured
  • Cerebral Cortex / drug effects*
  • Cerebral Cortex / metabolism
  • Electrophysiology
  • Neurons / cytology
  • Neurons / drug effects*
  • Neurons / metabolism
  • Piperidines / pharmacology*
  • Rats
  • Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*


  • Calcium Channels
  • Piperidines
  • Receptors, N-Methyl-D-Aspartate
  • eliprodil