Interaction of ibogaine with human α3β4-nicotinic acetylcholine receptors in different conformational states

Arias, Hugo R., Rosenberg, Avraham, Targowska-Duda, Katarzyna M., Feuerbach, Dominik, Yuan, Xiao Juan, Jozwiak, Krzysztof, Moaddel, Ruin, Wainer, Irving W. · 2010 · International Journal of Biochemistry & Cell Biology

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RECEPTOR MECHANISM: Ibogaine inhibits human α3β4 nAChRs with state-dependent binding - higher affinity for desensitised states. Noncompetitive mechanism supports nicotinic modulation as key anti-addiction pathway.

Dosing: Kd 0.46 µM; Ki 0.37 µM desensitised / 1.05 µM resting ([³H]ibogaine competition) (not-applicable)