Cell
May 11, 2023
Isha Singh, Anubha Seth, Christian B. Billesbølle et al.
97 citations
The serotonin transporter (SERT) removes synaptic serotonin and is the target of anti-depressant drugs. SERT adopts three conformations: outward-open, occluded, and inward-open. All known inhibitors target the outward-open state except ibogaine, which has unusual anti-depressant and substance-withdrawal effects, and stabilizes the inward-open conformation. Unfortunately, ibogaine's promiscuity...
Neuropharmacology
October 12, 2017
Felix P. Mayer, Nadine V. Burchardt, Ann M Decker et al.
30 citations
A variety of new psychoactive substances (NPS) are appearing in recreational drug markets worldwide. NPS are compounds that target various receptors and transporters in the central nervous system to achieve their psychoactive effects. Chemical modifications of existing drugs can generate NPS that are not controlled by current legislation, thereby providing legal alternatives to controlled...
Addiction Biology
March 1, 2014
Xaver Koenig, Michael Kovar, Stefan Boehm et al.
50 citations
Ibogaine, an alkaloid derived from the African shrub Tabernanthe iboga, has shown promising anti-addictive properties in animals. Anecdotal evidence suggests that ibogaine is also anti-addictive in humans. Thus, it alleviates drug craving and impedes relapse of drug use. Although not licensed as therapeutic drug, and despite evidence that ibogaine may disturb the rhythm of the heart, this...
The Journal of pharmacology and experimental therapeutics
February 1, 2014
Patrick Thurner, Anna Stary-Weinzinger, Hend Gafar et al.
41 citations
Ibogaine is a psychoactive indole alkaloid. Its use as an antiaddictive agent has been accompanied by QT prolongation and cardiac arrhythmias, which are most likely caused by human ether a go-go-related gene (hERG) potassium channel inhibition. Therefore, we studied in detail the interaction of ibogaine with hERG channels heterologously expressed in mammalian kidney tsA-201 cells. Currents...
Toxicology and Applied Pharmacology
December 1, 2013
Xaver Koenig, Michael Kovar, Lena Rubi et al.
46 citations
The plant alkaloid ibogaine has promising anti-addictive properties. Albeit not licensed as a therapeutic drug, and despite hints that ibogaine may perturb the heart rhythm, this alkaloid is used to treat drug addicts. We have recently reported that ibogaine inhibits human ERG (hERG) potassium channels at concentrations similar to the drugs affinity for several of its known brain targets....
BMC Pharmacology and Toxicology
September 1, 2012
Xaver Koenig, Michael Kovar, Lena Rubi et al.
The plant alkaloid ibogaine has shown promising anti-addictive properties in animals and humans. Although not licensed as a therapeutic drug, and despite evidence that ibogaine may disturb the rhythm of the heart, this alkaloid is used as an anti-addiction drug in alternative medicine. We have recently reported that therapeutic concentrations of ibogaine inhibit human ERG (hERG) potassium...
The Journal of biological chemistry
May 25, 2012
Simon Bulling, Klaus Schicker, Yuan-Wei Zhang et al.
124 citations
Ibogaine, a hallucinogenic alkaloid proposed as a treatment for opiate withdrawal, has been shown to inhibit serotonin transporter (SERT) noncompetitively, in contrast to all other known inhibitors, which are competitive with substrate. Ibogaine binding to SERT increases accessibility in the permeation pathway connecting the substrate-binding site with the cytoplasm. Because of the structural...
BMC Pharmacology
September 5, 2011
Michael Kovar, Xaver Koenig, Ágnes K. Mike et al.
5 citations
Background Ibogaine is an alkaloid derived from the African shrub Tabernanthe iboga. Psychoactive properties of ibogaine have been known for decades, but more recently the drug has received much attention because of its promising “anti-addictive” actions. Thus, ibogaine and its derivatives are being studied as potential treatment for opioid and stimulant abuse, as well as for alcoholism and...