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