European Journal of Pharmacology
June 6, 1995
W D Bowen, B J Vilner, W Williams et al.
95 citations
Ibogaine (12-methoxyibogamine) exhibited moderate affinity for sigma 2 sites (Ki = 201 nM) and low affinity for sigma 1 sites (Ki = 8554 nM), thus showing 43-fold selectivity for sigma 2 receptors. Tabernanthine (13-methoxyibogamine) and (+/-)-ibogamine had sigma 2 Ki = 194 nM and 137 nM, respectively. However, they showed 3- to 5-fold higher sigma 1 affinity compared to ibogaine, resulting in...
Neuroscience Letters
June 2, 1995
Deborah C. Mash, J K Staley, John Pablo et al.
82 citations
The putative anti-addiction alkaloid ibogaine and its principal metabolite 12-hydroxyibogamine appear to act at the (+)-5 methyl-10,11,dihydro-5H- dibenzo[a,d]cycloheten-5-10-imine maleate (MK-801) binding site in the N-methyl-D-aspartate (NMDA)-receptor cation channel. This conclusion is based on findings that both compounds competitively displaced specific [3H]MK-801 binding to membranes from...
Pharmacology
June 1, 1995
Robert V. House, P T Thomas, Hemendra N. Bhargava
12 citations
The immunomodulatory potential of the indole alkaloids ibogaine and harmaline was examined in a panel of in vitro immune function assays. These assays were chosen to assess T-cell regulatory and effector function, B-cell function, macrophage function, and natural killer-cell function. The in vitro exposure to either ibogaine or harmaline resulted in a dose-related suppression of all immune...
Pharmacology, Biochemistry, and Behavior
May 1, 1995
R P Kesner, P Jackson-Smith, C Henry et al.
25 citations
Ibogaine, a naturally occurring alkaloid, has been show to reduce naloxone-precipitated withdrawal symptoms from morphine. Given the clinical possibilities, it is important to determine ibogaine's effects on sensory-motor function, activity, learning, and memory. Long-Evans rats injected with doses of 20-60 mg/kg of ibogaine displayed slower response times on sensory and sensory-motor tests and...
Psychopharmacology
April 1, 1995
P M Sweetnam, Jack Lancaster, A Snowman et al.
109 citations
The indole alkaloid ibogaine (NIH 10567, Endabuse) is currently being examined for its potential utility in the treatment of cocaine and opioid addiction. However, a clearly defined molecular mechanism of action for ibogaine's putative anti-addictive properties has not been delineated. Radioligand binding assays targeting over 50 distinct neurotransmitter receptors, ion channels, and select...
Brain Research
March 27, 1995
S M Pearl, K Herrick-Davis, Milt Teitler et al.
78 citations
Radioligand-binding studies were performed to ascertain the actions of noribogaine, a suspected metabolite of ibogaine, on opioid receptors. Consistent with previous results, ibogaine showed highest affinity for kappa opioid receptors (Ki = 3.77 +/- 0.81 microM), less affinity for mu receptors (Ki = 11.04 +/- 0.66 microM) and no affinity for delta receptors (Ki > 100 microM). Noribogaine showed...
Psychopharmacology
February 1, 1995
S I Dworkin, S Gleeson, D Meloni et al.
49 citations
The effects of ibogaine (40 and 80 mg/kg, i.p.), an indole alkaloid proposed for the treatment of drug abuse, were determined in three different groups of rats responding under an FR10 schedule of food, cocaine or heroin reinforcement. Ibogaine (80 mg/kg, i.p.) given 60 min before the start of the session resulted in a 97% decrease in the number of ratios completed under the food reinforcement...
Life Sciences
1995
E E Codd
29 citations
The naturally occurring indole alkaloid ibogaine is of interest because of its reported ability to block drug seeking behavior for extended periods. The compound also potentiates morphine-induced analgesia in mice and reduces certain naltrexone-precipitated withdrawal signs in morphine-dependent rats. Although these results might suggest ibogaine interaction with opioid receptors, previous...
Life Sciences
1995
Deborah C. Mash, J K Staley, Michael H. Baumann et al.
108 citations
Ibogaine is a hallucinogenic indole with putative efficacy for the treatment of cocaine, stimulant and opiate abuse. The purported efficacy of ibogaine following single dose administrations has led to the suggestion that a long-acting metabolite of ibogaine may explain in part how the drug reduces craving for psychostimulants and opiates. We report here that 12-hydroxyibogamine, a primary...
Life Sciences
1995
R H Mach, C R Smith, S R Childers
145 citations
The alkaloid ibogaine is potentially useful to reduce craving for several drugs of abuse, but its mechanism of action is not known. In the current study, in vitro studies were conducted in order to determine the affinity of ibogaine for sigma receptors. Our results indicate that ibogaine has a relatively high affinity for sigma 2 receptors (Ki = 90.4 and 250 nM) and a significantly lower...