Ibogaine and the inhibition of acetylcholinesterase.
BACKGROUND
Ibogaine is a psychoactive monoterpine indole alkaloid extracted from the root bark of Tabernanthe iboga Baill. that is used globally in medical and nonmedical settings to treat drug and alcohol addiction, and is of interest as an ethnopharmacological prototype for experimental investigation and pharmaceutical development. The question of whether ibogaine inhibits acetylcholinesterase (AChE) is of pharmacological and toxicological significance.


METHODS
AChE activity was evaluated utilizing reaction with Ellman's reagent with physostigmine as a control.


RESULTS
Ibogaine inhibited AChE with an IC(50) of 520±40 μM.


CONCLUSIONS
Ibogaine's inhibition of AChE is physiologically negligible, and does not appear to account for observations of functional effects in animals and humans that might otherwise suggest the possible involvement of pathways linked to muscarinic acetylcholine transmission.
Department of Psychiatry, New York University School of Medicine, New York, NY 10016, USA. kra1@nyu.edu
Kenneth
K
Alper
Maarten E A
ME
Reith
Henry
H
Sershen
D000110:Acetylcholinesterase / Q000378:metabolism*; D000818:Animals; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D006801:Humans; D007050:Ibogaine / Q000494:pharmacology*; D010830:Physostigmine / Q000494:pharmacology; D024301:Plant Bark; D010936:Plant Extracts / Q000494:pharmacology*; D018517:Plant Roots; D030014:Tabernaemontana / Q000737:chemistry*
D002800:Cholinesterase Inhibitors; D010936:Plant Extracts; D007050:Ibogaine; D010830:Physostigmine; D000110:Acetylcholinesterase