Drug discrimination studies with ibogaine.
Scott Helsley, R A Rabin, Jerrold C Winter
The Alkaloids: Chemistry and Biology 2001 DOI: 10.1016/s0099-9598(01)56008-3 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Review Peer reviewed |
|---|---|
| Topics | Ibogaine |
| Keywords | Ibogaine compound Anti-addictive potential Therapeutic actions 5-ht2a 5-ht2c Sigma 2 Opiate receptors Mechanism Hallucinogens hallucinogenic properties |
| Citations | 4 |
| Key findings | Ibogaine's stimulus effects involve 5-HT2A, 5-HT2C, and sigma 2 receptors, with opiate receptors possibly involved, while sigma 1, PCP/MK-801, 5-HT3, and 5-HT1A receptors are not major contributors. |
Abstract
The results of the studies described here support the hypothesis that ibogaine produces its effects via selective interactions with multiple receptors. It appears that 5-HT2A, 5-HT2C, and sigma 2 receptors are involved in mediating the stimulus effects of ibogaine. In addition, opiate receptors may also be involved. In contrast, sigma 1, PCP/MK-801, 5-HT3, and 5-HT1A receptors do not appear to play a major role. Ibogaine's hallucinogenic effects may be explained by its interactions with 5-HT2A and 5-HT2C receptors, while its putative antiaddictive properties may result from its interactions with sigma 2 and opiate receptors. Alternatively, the possibility that ibogaine's hallucinogenic properties underlie its antiaddictive effects, as previously suggested (34), would support a role for 5-HT2 receptors in mediating the reported therapeutic effects of ibogaine. Certainly many questions remain regarding ibogaine's mechanism of action. Although drug discrimination will be useful for answering some of those questions, the true potential of this technique is realized whin it is combined with other techniques. The next few years promise to be fruitful with respect to our understanding of this agent. Reasons supporting this belief include advances in the study of sigma receptors, interest in ibogaine's effects on second messenger systems, and the development of ibogaine congeners such as 18-methoxycoronaridine (35). In conclusion, the aforementioned studies should serve to guide further endeavors. Pertinent questions have been generated: What is the role of sigma receptors in the effects of ibogaine, especially with regard to addiction? How does ibogaine affect opiate neurotransmission? What effects, if any, do the Harmala alkaloids have on addiction phenomena? What is the mechanism of action of harmaline? Can 10-hydroxyibogamine serve as a discriminative stimulus and, if so, what receptor interactions mediate its stimulus effects? Does the ibogaine-trained stimulus generalize to novel agents, including 18-methoxycoronaridine?
Comparable studies
Other narrative reviews on ibogaine, most cited first.
| Study | Year | Design | Participants |
|---|---|---|---|
| Psychedelics as medicines for substance abuse rehabilitation: evaluating treatments with LSD, Peyote, Ibogaine and Ayahuasca. | 2014 | Review | |
| The Anti-Addiction Drug Ibogaine and the Heart: A Delicate Relation Humans, animals | 2015 | Review | |
| Ibogaine in the treatment of substance dependence. | 2013 | Review | |
| Ibogaine, an anti-addictive drug: pharmacology and time to go further in development. A narrative review. | 2008 | Review | |
| Registered clinical studies investigating psychedelic drugs for psychiatric disorders. Registered clinical trials on clinicaltrials.gov evaluating psychedelics for... | 2021 | Review | n = 70 |
Citations in the library
Cited by 3
- Unique and potent effects of acute ibogaine on zebrafish: the developing utility of novel aquatic models for hallucinogenic drug research. Behavioural Brain Research 2013
- Ibogaine in the treatment of substance dependence. Current Drug Abuse Reviews March 1, 2013
- Chemical Interactions with Pyramidal Neurons in Layer 5 of the Cerebral Cortex: Control of Pain and Anxiety Current Medicinal Chemistry August 20, 2009
Cites 29
- Effects of iboga alkaloids on morphine and cocaine self-administration in rats: relationship to tremorigenic effects and to effects on dopamine release in nucleus accumbens and striatum. Brain Research September 19, 1994
- Ibogaine possesses a selective affinity for sigma 2 receptors. Life Sciences 1995
- Mechanisms of action of ibogaine and harmaline congeners based on radioligand binding studies. Brain Research February 7, 1992
- 18-Methoxycoronaridine, a non-toxic iboga alkaloid congener: effects on morphine and cocaine self-administration and on mesolimbic dopamine release in rats. Brain Research May 6, 1996
- Receptor binding profile suggests multiple mechanisms of action are responsible for ibogaine's putative anti-addictive activity. Psychopharmacology April 1, 1995
and 24 more in the library