Ibogaine and Noribogaine: Comparing Parent Compound to Metabolite
CNS Drug Reviews September 1, 2000 Peer reviewed DOI: 10.1111/j.1527-3458.2000.tb00149.x via OpenAlex
Summary
Ibogaine, a psychoactive compound from the Tabernanthe iboga shrub, has shown both acute and prolonged effects on neurochemistry and behavior. Its metabolite, noribogaine, produced after oral administration, is primarily responsible for its discriminative stimulus effects in rodents. Both compounds reduced morphine and cocaine intake, but ibogaine's neurotoxicity occurs at much higher doses than those proposed for human use. While clinical validation is lacking, ibogaine presents new avenues for drug addiction treatment research.
Study at a glance
| Population | rodents |
|---|---|
| Key finding | Noribogaine is primarily responsible for the discriminative stimulus effects of ibogaine in rodents. |
Abstract
ABSTRACT Ibogaine is one of the psychoactive alkaloids found in the West African shrub Tabernanthe iboga. Since the 1980s, a series of US patents have claimed efficacy for ibogaine in the treatment of drug addiction. Since then, more than 60 scientific publications on ibogaine and drug addiction have been published. Ibogaine has an acute and a prolonged effect on neurochemistry and behavior. Its metabolite, noribogaine (12‐hydroxyibogamine), is produced through metabolic demethylation soon after oral ibogaine administration. Although, they share similar chemical structures, ibogaine and noribogaine display different binding profiles. In rodents both, ibogaine and noribogaine, decreased morphine and cocaine intake and modulated dopaminergic transmission. In rats trained to discriminate ibogaine from saline, complete generalization to noribogaine was obtained. Attempts to correlate brain levels of both, the parent compound and the metabolite indicate that noribogaine is primarily responsible for ibogaine discriminative stimulus. Ibogaine‐induced neurotoxicity tends to occur at doses much higher than the proposed dose for humans, but caution is important when extrapolating data from ibogaine's effects observed in rodents. Although a definitive clinical validation of purported ibogaine effects is still unavailable, ibogaine has opened new perspectives in the investigation of pharmacotherapies for drug addiction.