Ibogaine: a potent noncompetitive blocker of ganglionic/neuronal nicotinic receptors.
Molecular pharmacology January 1, 1997 B Badio, W L Padgett, J W Daly 52 citations
Ibogaine blocks a specific type of nicotinic receptor channel (ganglionic type) in rat cells, with an IC50 around 20 nM. Its main metabolite, O-des-methylibogaine, is 75 times less potent, and a modified version is 20 times less potent. Ibogaine is much weaker at blocking neuromuscular-type nicotinic receptors. The blockade in rat cells is only partially reversible. In mice, a 10 mg/kg dose of ibogaine completely blocks pain relief caused by epibatidine, which acts through central nicotinic receptors. This effect is gone 24 hours after a 40 mg/kg dose. Blocking these channels may contribute to ibogaine's anti-addictive properties.