Ibogaine possesses a selective affinity for sigma 2 receptors.
R H Mach, C R Smith, S R Childers
Life Sciences 1995 DOI: 10.1016/0024-3205(95)00301-l (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | In vitro study Peer reviewed |
|---|---|
| Population | In vitro (receptor binding) |
| Topics | Ibogaine |
| Citations | 145 |
| Key points | Ibogaine has a relatively high affinity for sigma-2 receptors and a significantly lower affinity for sigma-1 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 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.