100 years of ibogaine: neurochemical and pharmacological actions of a putative anti-addictive drug.
Pharmacological Reviews June 1, 1995 P Popik, R T Layer, P Skolnick 185 citations
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R T Layer
Laboratory of Neuroscience, National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0008, USA. rtlayer@helix.nih.gov
3 papers in the library · 325 citations · publishing 1994-1996
Papers
The putative anti-addictive drug ibogaine is a competitive inhibitor of [3H]MK-801 binding to the NMDA receptor complex.
Psychopharmacology May 1, 1994 P Popik, R T Layer, P Skolnick 92 citations
Ibogaine, a potential treatment for addiction to opiates, stimulants, and alcohol, acts as a competitive inhibitor of NMDA receptor coupled cation channels, binding to the same site as MK-801. This suggests that ibogaine's ability to reduce drug-seeking behavior in humans may stem from blocking these channels, similar to how MK-801 prevents tolerance to morphine and alcohol and reduces sensitization to stimulants in animal studies.
Structurally modified ibogaine analogs exhibit differing affinities for NMDA receptors.
European journal of pharmacology August 8, 1996 R T Layer, P Skolnick, C M Bertha et al. 48 citations
Ibogaine, a psychoactive alkaloid, is more potent than its analogs at blocking NMDA receptors, a brain target linked to addiction. In lab tests, ibogaine inhibited [3H]MK-801 binding to NMDA receptors most strongly (Ki ≈ 1.2 µM), while similar compounds like O-desmethylibogaine were less potent (Ki ≈ 5.5 µM) and O-t-butyl-O-desmethylibogaine much weaker (Ki ≈ 179 µM). In morphine-dependent mice, only ibogaine reduced withdrawal jumping triggered by naloxone, suggesting its anti-addictive effects stem from NMDA receptor antagonism.