Receptor binding profile suggests multiple mechanisms of action are responsible for ibogaine's putative anti-addictive activity

P. M. Sweetnam, J. Lancaster, Adele Snowman, J. L. Collins, S. Perschke, C. Bauer, J. Ferkany

Research output: Contribution to journalArticle

Abstract

The indole alkaloid ibogaine (NIH 10567, Endabuse) is currently being examined for its potential utility in the treatment of cocaine and opioid addiction. However, a clearly defined molecular mechanism of action for ibogaine's putative anti-addictive properties has not been delineated. Radioligand binding assays targeting over 50 distinct neurotransmitter receptors, ion channels, and select second messenger systems were employed to establish a broad in vitro pharmacological profile for ibogaine. These studies revealed that ibogaine interacted with a wide variety of receptors at concentrations of 1-100 μM. These included the mu, delta, kappa, opiate, 5HT2, 5HT3, and muscarinic1 and 2 receptors, and the dopamine, norepinephrine, and serotonin uptake sites. In addition, ibogaine interacted with N-methyl-d-aspartic acid (NMDA) associated ion and sodium ion channels as determined by the inhibition of [3H]MK-801 and [3H]bactrachotoxin A 20-α-benzoate binding (BTX-B), respectively. This broad spectrum of activity may in part be responsible for ibogaine's putative anti-addictive activity.

Original languageEnglish (US)
Pages (from-to)369-376
Number of pages8
JournalPsychopharmacology
Volume118
Issue number4
DOIs
StatePublished - Apr 1 1995
Externally publishedYes

Keywords

  • Addiction
  • Drug abuse
  • Ibogaine
  • Neurotransmitter receptors
  • Radioligand binding

ASJC Scopus subject areas

  • Pharmacology

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