The putative anti-addictive drug ibogaine is a competitive inhibitor of [3H]MK-801 binding to the NMDA receptor complex

Psychopharmacology (Berl). 1994 May;114(4):672-4. doi: 10.1007/BF02245000.

Abstract

Ibogaine is a putative anti-addictive drug with potential efficacy for the treatment of opiate, stimulant, and alcohol abuse. We now report ibogaine is a competitive inhibitor (Ki, 1.01 +/- 0.1 microM) of [3H]MK-801 binding to N-methyl-D-aspartate (NMDA) receptor coupled cation channels. Since MK-801 can attenuate the development of tolerance to morphine and alcohol as well as sensitization to stimulants in preclinical studies, the reported ability of ibogaine to modify drug-seeking behavior in man may be attributable to a blockade of NMDA receptor coupled cation channels.

MeSH terms

  • Animals
  • Binding, Competitive / drug effects
  • Dizocilpine Maleate / antagonists & inhibitors
  • Dizocilpine Maleate / pharmacokinetics*
  • Ibogaine / pharmacology*
  • In Vitro Techniques
  • Ion Channels / drug effects
  • Ion Channels / metabolism
  • Ligands
  • Phencyclidine / analogs & derivatives
  • Phencyclidine / pharmacology
  • Rats
  • Receptors, Glutamate / drug effects
  • Receptors, Glutamate / metabolism
  • Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors
  • Receptors, N-Methyl-D-Aspartate / metabolism*

Substances

  • Ion Channels
  • Ligands
  • Receptors, Glutamate
  • Receptors, N-Methyl-D-Aspartate
  • Ibogaine
  • Dizocilpine Maleate
  • tenocyclidine
  • Phencyclidine