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0026-895X/97/010001-05$3.00/0
Copyright © by The American Society for Pharmacology and Experimental Therapeutics
All rights of reproduction in any form reserved.
MOLECULAR PHARMACOLOGY 51:1-5 (1997).


ACCELERATED COMMUNICATION
Ibogaine: A Potent Noncompetitive Blocker of Ganglionic/Neuronal Nicotinic Receptors

Barbara Badio, William L. Padgett, and John W. Daly

Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892-0820

Ibogaine noncompetitively blocked (IC50 ~ 20 nM) 22NaCl influx through ganglionic-type nicotinic receptor channels of rat pheochromocytoma PC12 cells. The major metabolite O-desmethylibogaine was 75-fold less active, and O-t-butyl-O-desmethylibogaine was 20-fold less active. Ibogaine was relatively weak as a blocker (IC50 ~ 2000 nM) of the neuromuscular-type nicotinic receptor channels in human medulloblastoma TE671 cells. The blockade of nicotinic responses by ibogaine was only partially reversible in PC12 cells. In vivo, ibogaine at 10 mg/kg completely blocked epibatidine-elicited antinociception in mice, a response that is mediated by central nicotinic receptor channels. There was no significant blockade of the epibatidine response at 24 hr after the administration of 40 mg/kg ibogaine. The blockade of nicotinic channels could contribute to the antiaddictive properties of ibogaine.

Copyright © by The American Society for Pharmacology and Experimental Therapeutics


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