Interaction of ibogaine analogs with the nicotinic acetylcholine receptor
The FASEB Journal April 1, 2008 Krzysztof Jóźwiak, Ruin Moaddel, Irving W. Wainer et al. 2 citations
Ibogaine analogs, especially 18-methoxycoronaridine (18-MC), bind to a specific site within the ion channel of the nicotinic acetylcholine receptor (AChR) when the receptor is in a desensitized state. The affinity of 18-MC for this site is about 0.17 μM in the desensitized state, much higher than in the resting state (12 μM). The binding site overlaps with the TCP locus, located between valine and leucine rings in the channel. These compounds enhance binding of the agonist cytisine only when the receptor is in a resting but activable state, not when desensitized. The findings suggest that ibogaine analogs inhibit the AChR by promoting receptor desensitization.