Interaction of narcotic antagonist naltrexone with nicotinic acetylcholine receptor

European Journal of Pharmacology
L OliveiraE X Albuquerque


The interactions of naltrexone with the nicotinic acetylcholine receptor were studied electrophysiologically using the frog sciatic nerve-sartorius muscle and biochemically using membranes from the electric organ of Torpedo ocellata. At nanomolar concentrations naltrexone increased the peak amplitude of endplate currents with little change in the decay time constant. At micromolar concentrations there was a concentration-dependent depression of endplate current and miniature endplate current amplitudes and decay time constants. Decay time constant depression was enhanced with hyperpolarization. Only marginal curvature was induced in peak endplate current amplitude versus membrane voltage plots by naltrexone. Naltrexone had no effect on single channel conductance but decreased open channel lifetime, according to fluctuation analysis. Naltrexone alone (less than or equal to 3 microM) did not impair binding of [125I]alpha-bungarotoxin to the receptor in a fast pre-equilibration assay, but increased the ability of acetylcholine to displace [125I]alpha-bungarotoxin. The drug displaced the agonist-stimulated binding of [3H]perhydrohistrionicotoxin to the channel site. Biphasic functional changes in neuromuscular transmission can be a...Continue Reading


Nov 5, 1979·Life Sciences·J SawynokF S LaBella
May 1, 1977·Proceedings of the National Academy of Sciences of the United States of America·A T EldefrawiB Witkop
Sep 1, 1978·The Journal of General Physiology·L M Masukawa, E X Albuquerque
May 1, 1986·Proceedings of the National Academy of Sciences of the United States of America·L G AguayoE X Albuquerque
Feb 1, 1985·Proceedings of the National Academy of Sciences of the United States of America·R E OswaldJ T McLaughlin
May 19, 1971·Nature: New Biology·C Pinsky, R C Frederickson
Feb 1, 1974·Analytical Biochemistry·M K Lewis, M E Eldefrawi
Mar 6, 1981·Proceedings of the Royal Society of London. Series B, Containing Papers of a Biological Character·D Colquhoun, A G Hawkes
Feb 1, 1984·The Journal of Physiology·D E Clapham, E Neher
Jan 1, 1980·Annals of the New York Academy of Sciences·E X AlbuquerqueL Aguayo
Jan 1, 1980·Annals of the New York Academy of Sciences·M E Eldefrawi, A T Eldefrawi
Jan 1, 1984·Biophysical Journal·S M Sine, J H Steinbach
Sep 21, 1984·Science·J P ChangeuxP Chemouilli
Jan 1, 1983·Life Sciences·A A BadawyC J Morgan
Jan 1, 1984·Ophthalmologica. Journal international d'ophtalmologie. International journal of ophthalmology. Zeitschrift für Augenheilkunde·J François
Mar 1, 1994·Epilepsia·B E Swartz
Apr 29, 1998·Trends in Pharmacological Sciences·S D BryantL H Lazarus

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