NMDA-receptor antagonism via dextromethorphan and ifenprodil modulates graded anxiety test performance of C57BL/6 mice

Behav Pharmacol. 2003 May;14(3):245-9. doi: 10.1097/00008877-200305000-00009.

Abstract

The majority of N-methyl-D-aspartate receptors (NMDA-R) in the adult forebrain are di- or triheteromers composed of NR1, NR2A and NR2B subunits. Subunit non-selective NMDA-R antagonists produce anxiolytic-like effects together with motor and sensory side-effects. The graded anxiety test (GAT), permits the within-task distinction of drug effects on anxiety from those on activity and perception. By testing NMDA-R subunit selective agents in the GAT it might be possible to determine whether their effects on anxiety, activity and perception are interrelated, and whether separate NMDA-R subtypes are involved. Dextromethorphan (weakly NR2A-selective) (10 and 30 mg/kg, i.p.) and ifenprodil (highly NR2B-selective) (1, 3 and 5 mg/kg, i.p.) were tested in the GAT. Both drugs failed to induce anxiolysis devoid of side-effects. However, the 10 mg/kg dose of dextromethorpan showed an anxiolytic, whereas the 30 mg/kg dose showed an anxiogenic, behavioral profile. Since the selective blockade of the NR2B subunit by ifenprodil had no clear anxiolytic effect, the anxiolytic potential of NMDA subunit non-selective agents might involve NR2A-containing receptors.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anxiety / psychology*
  • Attention / drug effects
  • Darkness
  • Dextromethorphan / pharmacology*
  • Light
  • Male
  • Maze Learning / drug effects
  • Mice
  • Mice, Inbred C57BL
  • Motor Activity / drug effects
  • Piperidines / pharmacology*
  • Protein Subunits
  • Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*

Substances

  • NR2A NMDA receptor
  • NR2B NMDA receptor
  • Piperidines
  • Protein Subunits
  • Receptors, N-Methyl-D-Aspartate
  • Dextromethorphan
  • ifenprodil