Ibogaine possesses a selective affinity for σ2 receptors

Abstract

The alkaloid ibogaine is potentially useful to reduce craving for several drugs of abuse, but its mechanism of action is not known. In the current study, in vitro studies were conducted in order to determine the affinity of ibogaine for sigma receptors. Our results indicate that ibogaine has a relatively high affinity for σ 2 receptors (K i = 90.4 and 250 nM) and a significantly lower affinity for σ 1 receptors (K i = 9310 nM). These data suggest that ibogaine may have a higher affinity at σ 2 receptors than any other known CNS receptor. Its low affinity for σ 1 receptors also suggests that ibogaine may be a suitable lead compound for structure-activity relationship studies aimed at developing σ 2-selective ligands.