The putative anti-addictive drug ibogaine is a competitive inhibitor of [3H]MK-801 binding to the NMDA receptor complex.
P Popik, R T Layer, P Skolnick
Psychopharmacology May 1, 1994 DOI: 10.1007/bf02245000 via PubMed
Summary
AI-generated from the abstractIbogaine, 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.
Study at a glance
| Characteristics | Laboratory study Peer reviewed |
|---|---|
| Population | Cells |
| Citations | 92 |
| Key finding | Ibogaine is a competitive inhibitor of NMDA receptor coupled cation channels, which may explain its anti-addictive properties. |
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.