Annals of the New York Academy of Sciences
September 1, 2000
D C Mash, C A Kovera, J Pablo et al.
146 citations
Ibogaine, an indole alkaloid from the Tabernanthe Iboga shrub, has been used in low doses by indigenous peoples to combat fatigue, hunger, and thirst, and in higher doses as a religious sacrament. Anecdotal reports from addict self-help groups claim a single dose eliminates opiate withdrawal symptoms and reduces drug craving for extended periods. The compound is rapidly metabolized via CYP2D6 into noribogaine, which may underlie its prolonged effects. In an inpatient detoxification setting, ibogaine significantly decreased craving for cocaine and heroin and reduced self-reported depressive symptoms, with benefits persisting 30 days after discharge. The findings suggest noribogaine's central nervous system activity may explain the lasting aftereffects on craving and mood.
Psychopharmacology
September 1, 1996
J K Staley, Q Ouyang, J Pablo et al.
82 citations
Ibogaine, a treatment for drug dependence, is metabolized into 12-hydroxyibogamine (12-OH ibogamine). Both the parent drug and metabolite bind to similar molecular targets, with the highest potency at the cocaine recognition site on the serotonin transporter. The metabolite shows higher affinity at the kappa-1 receptor and lower affinity at the NMDA receptor compared to ibogaine. Micromolar concentrations of both compounds are found in rat brain. The combined actions of ibogaine and its metabolite at key pharmacological targets may alter drug-seeking behavior by modulating reward circuits.
Journal of analytical toxicology
October 1, 1995
W L Hearn, J Pablo, G W Hime et al.
44 citations
A sensitive method was developed to measure ibogaine and its major metabolite, 12-hydroxy-ibogamine (noribogaine), in biological fluids and brain tissue. The metabolite was identified using gas chromatography-mass spectrometry. The procedure involves solvent extraction, derivatization with ethyl iodide, and cleanup before analysis. Detection limits were 5 ng/mL for both compounds, and quantitation limits ranged from 5 to 10 ng/mL across all tested matrices. Calibration curves were linear from 3 to 1000 ng/mL or ng/g.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology
July 1, 1999
C Zubaran, M Shoaib, I P Stolerman et al.
31 citations
In rats trained to distinguish ibogaine from a placebo, the metabolite noribogaine produced the same discriminative effect as ibogaine but at roughly half the dose. Noribogaine was found in blood and brain tissue after either ibogaine or noribogaine was given. At doses that produced the discriminative effect, noribogaine concentrations in plasma, cerebral cortex, and striatum were similar whether ibogaine or noribogaine was administered. The findings suggest noribogaine may lack the NMDA antagonist and kappa-opioid agonist effects of ibogaine and may be primarily responsible for ibogaine's discriminative stimulus effect in rats.