Differential effects of ketamine enantiomers on NMDA receptor currents in cultured neurons

Eur J Pharmacol. 1992 Mar 17;213(1):155-8. doi: 10.1016/0014-2999(92)90248-3.


The effects of R- and S-ketamine on N-methyl-D-aspartate receptor-activated cation currents (NMDA receptor currents) of voltage-clamped cultured rat hippocampal neurons were investigated using the whole-cell patch-clamp technique. Both enantiomers exhibited a voltage- and use-dependent blockade of NMDA receptor currents, with the S-enantiomer being about twice as potent as the R-enantiomer. Calculated relative forward and backward rates suggest that conformational differences influence the dissociation from the binding site more than the association with it.

MeSH terms

  • Animals
  • Binding Sites
  • Cells, Cultured
  • Hippocampus / cytology
  • Hippocampus / drug effects
  • Hippocampus / physiology
  • Ketamine / administration & dosage
  • Ketamine / pharmacology*
  • Membrane Potentials / drug effects
  • Neurons / drug effects
  • Neurons / physiology*
  • Rats
  • Rats, Inbred Strains
  • Receptors, N-Methyl-D-Aspartate / drug effects*
  • Receptors, N-Methyl-D-Aspartate / metabolism
  • Stereoisomerism


  • Receptors, N-Methyl-D-Aspartate
  • Ketamine