Mechanism of hERG Channel Block by the Psychoactive Indole Alkaloid Ibogaine

Thurner, Patrick, Stary-Weinzinger, Anna, Gafar, Hend, Gawali, Vaibhavkumar S., Kudlacek, Oliver, Zezula, Juergen, Hilber, Karlheinz, Boehm, Stefan, Sandtner, Walter, Koenig, Xaver · 2014 · Journal of Pharmacology and Experimental Therapeutics

AI-extracted · unverified · confirm at source

hERG IC₅₀ ~1.0 μM (Fig 5C tail) and ~1.2 μM (Fig 5B sustained at +10 mV); ~3–4 μM figures elsewhere cite Koenig 2012/2013. Y652A 5-fold + F656A 50-fold reductions. Best fit OIB; closed-state binding negligible (COIB null vs OIB, P>0.05).

Dosing: IC₅₀ ~1.0–1.2 μM (hERG wild-type, this paper's protocols); 3 μM standard test concentration — in vitro (not-applicable)

Safety data present: HERG