Ibogaine and the inhibition of acetylcholinesterase.
Kenneth Alper, Maarten E.A. Reith, Henry Sershen
Journal of Ethnopharmacology February 15, 2012 DOI: 10.1016/j.jep.2011.12.006 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Experimental study Peer reviewed |
|---|---|
| Intervention | Ibogaine |
| Topics | Ibogaine |
| Keywords | Acetylcholinesterase inhibition Drug safety |
| Citations | 13 |
| Key findings | Ibogaine inhibits acetylcholinesterase with an IC50 of 520 ± 40 μM, but this inhibition is physiologically negligible and does not account for observed functional effects in animals and humans. |
Abstract
Ibogaine is a psychoactive monoterpine indole alkaloid extracted from the root bark of Tabernanthe iboga Baill. that is used globally in medical and nonmedical settings to treat drug and alcohol addiction, and is of interest as an ethnopharmacological prototype for experimental investigation and pharmaceutical development. The question of whether ibogaine inhibits acetylcholinesterase (AChE) is of pharmacological and toxicological significance. AChE activity was evaluated utilizing reaction with Ellman's reagent with physostigmine as a control. Ibogaine inhibited AChE with an IC(50) of 520±40 μM. Ibogaine's inhibition of AChE is physiologically negligible, and does not appear to account for observations of functional effects in animals and humans that might otherwise suggest the possible involvement of pathways linked to muscarinic acetylcholine transmission.
Comparable studies
Other experimental studies on ibogaine, most cited first.
| Study | Year | Design | Participants |
|---|---|---|---|
| Ibogaine, a noncompetitive inhibitor of serotonin transport, acts by stabilizing the cytoplasm-facing state of the transporter. In vitro (SERT) | 2007 | Laboratory study | |
| Mechanisms of action of ibogaine and harmaline congeners based on radioligand binding studies. | 1992 | Laboratory study | |
| The mechanistic basis for noncompetitive ibogaine inhibition of serotonin and dopamine transporters. | 2012 | Experimental study | |
| Identification of a primary metabolite of ibogaine that targets serotonin transporters and elevates serotonin. | 1995 | Experimental study | |
| Ibogaine and its congeners are sigma 2 receptor-selective ligands with moderate affinity. | 1995 | Laboratory study |
Citations in the library
Cited by 5
- The Anti-Addiction Drug Ibogaine and the Heart: A Delicate Relation Molecules January 29, 2015
- Fatalities temporally associated with the ingestion of ibogaine. Journal of Forensic Sciences March 1, 2012
- The Iboga Alkaloids. Progress in the chemistry of organic natural products 2017
- hERG Blockade by Iboga Alkaloids. Cardiovascular toxicology 2016
- Mexican calea (Calea zacatechichi Schltdl.) interferes with cholinergic and dopaminergic pathways and causes neuroglial toxicity. Journal of Ethnopharmacology January 30, 2025
Cites 14
- Treatment of acute opioid withdrawal with ibogaine. American Journal on Addictions 1999
- The ibogaine medical subculture. Journal of Ethnopharmacology January 4, 2008
- Ibogaine: complex pharmacokinetics, concerns for safety, and preliminary efficacy measures. Annals of the New York Academy of Sciences September 1, 2000
- Mechanisms of action of ibogaine and harmaline congeners based on radioligand binding studies. Brain Research February 7, 1992
- Receptor binding profile suggests multiple mechanisms of action are responsible for ibogaine's putative anti-addictive activity. Psychopharmacology April 1, 1995
and 9 more in the library