Ibogaine possesses a selective affinity for sigma 2 receptors.
Life sciences – January 01, 1995
Source: PubMed
Summary
Ibogaine shows promise in reducing cravings for various drugs, primarily due to its strong binding to sigma 2 receptors. In a study with detailed in vitro analyses, ibogaine exhibited a high affinity for sigma 2 receptors (Ki = 90.4 and 250 nM) compared to a much lower affinity for sigma 1 receptors (Ki = 9310 nM). This suggests that ibogaine could be an effective lead compound for developing targeted treatments focused on sigma 2-selective ligands, potentially enhancing therapeutic options for addiction.
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 sigma 2 receptors (Ki = 90.4 and 250 nM) and a significantly lower affinity for sigma 1 receptors (Ki = 9310 nM). These data suggest that ibogaine may have a higher affinity at sigma 2 receptors than any other known CNS receptor. Its low affinity for sigma 1 receptors also suggests that ibogaine may be a suitable lead compound for structure-activity relationship studies aimed at developing sigma 2-selective ligands.