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Ibogaine and Its Congeners Are σ Receptor-Selective Ligands with Moderate Affinity

Bowen, Wayne D., Vilner, Bertold J., Williams, Wanda, Bertha, Craig M., Kuehne, Martin E., Jacobson, Arthur E. · 1995 · European Journal of Pharmacology

Mechanisms In vitro moderate

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Ibogaine binds σ₂ receptors (Kᵢ = 201 nM) with 43-fold selectivity over σ₁ — highest affinity target known at time. O-desmethylibogaine loses σ₂ affinity (Kᵢ = 5226 nM), suggesting demethylation terminates σ-mediated effects.

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