Antidepressant-like actions of the polyamine site NMDA antagonist, eliprodil (SL-82.0715)

Pharmacol Biochem Behav. 1995 Nov;52(3):621-7. doi: 10.1016/0091-3057(95)00155-p.

Abstract

Functional N-methyl-D-aspartate (NMDA) antagonists including competitive antagonists, glycine partial agonists, and use-dependent channel blockers exhibit antidepressant-like actions in preclinical models. The present study examined the effects of eliprodil (SL-82.0715), an NMDA antagonist acting at polyamine sites, in behavioral and neurochemical tests predictive of antidepressant activity. In mice, eliprodil produced a dose-dependent reduction in immobility in the forced swim test, but was inactive in the tail suspension test. Chronic treatment with eliprodil produced both a significant downregulation of beta-adrenoceptors and a reduction in the potency of glycine to inhibit [3H]5,7-dichlorokynurenic acid binding to strychnine-insensitive glycine receptors in neocortical membranes. In toto, these data indicate that like other NMDA antagonists, eliprodil possesses antidepressant-like actions in preclinical tests predictive of clinical efficacy.

MeSH terms

  • Adrenergic Uptake Inhibitors / pharmacology
  • Adrenergic beta-Antagonists / pharmacology
  • Animals
  • Antidepressive Agents / pharmacology*
  • Behavior, Animal / drug effects
  • Biogenic Polyamines / metabolism*
  • Brain Chemistry / drug effects
  • Down-Regulation / drug effects
  • Excitatory Amino Acid Antagonists / pharmacology*
  • Glycine / antagonists & inhibitors
  • Glycine / pharmacology
  • Imipramine / pharmacology
  • Kynurenic Acid / analogs & derivatives
  • Kynurenic Acid / antagonists & inhibitors
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Motor Activity / drug effects
  • Piperidines / pharmacology*
  • Receptors, Glycine / antagonists & inhibitors

Substances

  • Adrenergic Uptake Inhibitors
  • Adrenergic beta-Antagonists
  • Antidepressive Agents
  • Biogenic Polyamines
  • Excitatory Amino Acid Antagonists
  • Piperidines
  • Receptors, Glycine
  • Kynurenic Acid
  • Imipramine
  • 5,7-dichlorokynurenic acid
  • Glycine
  • eliprodil