Ibogaine block of the NMDA receptor: in vitro and in vivo studies.
Neuropharmacology April 1, 1996 K Chen, T G Kokate, S D Donevan et al. 55 citations
Ibogaine, a hallucinogenic alkaloid claimed to reduce addiction, blocks NMDA receptors in the brain. In cultured rat hippocampal neurons, ibogaine slowly and reversibly blocked NMDA-induced currents with an IC50 of 3.1 µM at −60 mV, while not affecting kainate or GABA currents. The block was use- and voltage-dependent and could be occluded by magnesium. Ibogaine also inhibited dizocilpine binding to NMDA receptors in rat forebrain membranes (IC50, 3.2 µM). In mice, ibogaine fully protected against maximal electroshock seizures (ED50, 31 mg/kg, i.p.) and partially protected against NMDA-induced lethality, confirming in vivo NMDA receptor blockade.