The putative anti-addictive drug ibogaine is a competitive inhibitor of [3H]MK-801 binding to the NMDA receptor complex.
Psychopharmacology – May 01, 1994
Source: PubMed
Summary
Ibogaine shows promise as an anti-addictive drug, potentially altering drug-seeking behavior. In a study with competitive inhibition measured at a Ki of 1.01 µM, ibogaine effectively blocked [3H]MK-801 binding to NMDA receptor channels. This mechanism is significant because MK-801 has been shown to reduce tolerance to morphine and alcohol and prevent stimulant sensitization in preclinical models. These findings suggest that ibogaine's impact on addiction may be linked to its action on these critical receptors.
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.