THE PUTATIVE ANTI-ADDICTIVE DRUG IBOGAINE IS A COMPETITIVE INHIBITOR OF [H-3] MK-801 BINDING TO THE NMDA RECEPTOR COMPLEX

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 (K-i, 1.01 +/- 0.1 mu M) of [H-3]M K-801 binding to N-methyl-D-aspartate (NMDA) receptor coupled cation c hannels. Since MK-801 can attenuate the development of tolerance to mo rphine and alcohol as well as sensitization to stimulants in preclinic al studies, the reported ability of ibogaine to modify drug-seeking be havior in man may be attributable to a blockade of NMDA receptor coupl ed cation channels.