Abstract
Opioid pure agonists, morphine, meperidine and methadone, were used to investigate the effect on the opioid receptor of frog sciatic nerve fibers using sucrose gap apparatus. When applied extracellularly by perfusion, morphine, methadone and meperidine significantly depressed the amplitude of the action potential in frog sciatic nerve fibers as a dose-dependent (10−10 M-10−2 M) manner. The depression with morphine or methadone was partially antagonized by the simultaueous treatment with a lower (10−10 M-10−8 M) concentration of naloxone, but that of meperidine was not blocked. When the three opioid agonists were applied intracellularly by placing it in a compartment with a cut end of the sciatic nerve fibers, all of them depressed the amplitude of the action potentials by similar potency, and there reductions significantly blocked by pretreatment of lower concentration (10−10 M-10−8 M) of naloxone. These results support the previous findings by other workers that the stereospecific opioid receptors of this preparation are located on or near the intracellular opening of the sodiumchannels which are sensitive to naloxone.
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References Cited
Ariens, E. J., van Rossum, J. M. and Simonis, A. M., Affinity, intrinsic activity and drug interaction.Pharmacol. Rev., 9, 218–236 (1957).
Ary, T. E. and Frank, G. B., Streospecificity of an opiate action on the excitable membrane of frog skeletal muscle fibres.Eur. J. Pharmacol., 94, 211–217 (1983).
France, C. P., Jacobson, A. E. and Woods, J. H., Discriminative stimulus effects of reversible and irreversible opiate agonist: morphine, oxymorphazone and buprenorphine.J. Pharmacol. Exp. Ther., 230, 652–657 (1984).
Frank, G. B., Drugs which modify membrane excitability.Fed. Proc., 27, 132–136 (1968).
Frank, G. B., Two mechanisms for the meperidine block of action potential: nonspecific and opiate drug receptor mediated blockade.J. Physiol. (London), 252, 585–601 (1975).
Frank, G. B., Stereospecific opiod drug receptors on excitable cell membranes.Can. J. Physiol. Pharmacol., 63, 1023–1032 (1985).
Frank, G. B. and Buttar, H. S., Effects of morphine and meperidine on action potentials production in frog's skeletal muscle fibers.Can. J. Physiol. Pharmacol., 53, 92–96 (1975).
Frank, G. B. and Marwaha, J., An investigation of the activity of opiate drug receptors located on the frog's skeletal muscle fibre membrane.Can. J. Physiol. Pharmacol., 56, 501–508 (1978).
Frank, G. B., and Marwaha, J., Naloxone and naltrexone: actions and interactions at an opiate drug receptor on frog skeletal muscle fibers.J. Pharmacol. Exp. Ther., 209, 382–388 (1979).
Frank, G. B., and Sudha T. S., Effects of enkephalin applied intracellularly, on action potentials in vertebrated A and C nerve fibre axons.Neuropharmacology, 26(1), 61–66 (1987).
Frazier, D. T., Murayama, K., Abbott, N. J. and Narahashi, T., Effects of morphine on internally perfused squid giant axon.Proc. Soc. Exp. Biol. Med., 139, 434–438 (1972).
Hodgkin, A. L. and Katz, B., The effect of sodium ions on the electrical activity of the giant axon of the squid.J. Physiol. (London), 108, 37–77 (1949).
Hu, S., and Rubly, N., Effects of morphine on ionic currents in frog node of Ranvier.Eur. J. Pharmacol., 95, 185–192 (1983).
Hunter, E. G., and Frank, G. B., An opiate receptor on frog sciatic nerve axons.Can. J. Physiol. Pharmacol., 57, 1171–1174 (1979).
Jurna, I. and Grossman, W., The effect of morphine on mammalian nerve fibers.Eur. J. Pharmacol., 44, 339–348 (1977).
Kosterlitz, H. W., and Wallis, E. I., The action of morphine-like drugs on impulse transmission in mammalian nerve fibers.Br. J. Pharmacol., 22, 499–501 (1964).
Lee, J. H. and Frank, G. B., Agonist-antagonist effects of buprenorphine on action potentials of frog sciatic nerve fibers.Kor. J. Pharmacol., 25, 23–30 (1989a).
Lee, J. H., and Frank, G. B., Opioid effects of racemic ketamine on the excitablity of sciatic nerve and skeletal muscle fibers of the frog.Jap. J. Pharmacol., 51, 321–327 (1989b).
Martin, W. R., Eades, C. G., Thomson, J. A., Huppler, R. E. and Gilbert, P. E., The effects of morphine-and nalorphine-like drugs in the nondependent and morphine-dependent chronic spinal dog.J. Pharmacol. Exp. Ther., 197, 517–532 (1976).
McFadzean, I., The ionic mechanisms underlying opioid actions.Neuropeptides, 11, 173–180 (1988).
North, R. A., Opioid receptor types and membrane ion channels.TINS, 114–117 (1986).
Rance, M. J., Animal and molecular pharmacology of mixed agonist-antagonist analgesic drugs.Br. J. Clin. Pharmacol., 7, 2815–2865 (1979).
Seeman, P., Chau-Wong, M., and Moyyen, S., Identical effects of levo- and dextro-forms.Can. J. Physiol. Pharmacol., 50, 1181–1192 (1972).
Shefner, S.A., North, N.A. and Zukin, P.S., Opiate effects on rabbit vagus nerve: electrophysiology and radioligand binding.Brain Research, 221, 109–116 (1981).
Simon, E. J., and Rosenberg, P., Effects of narcotics on the giant axon of the squid.J. Neurochem., 17, 881–887 (1970).
Smuda, J. W. and Levie, R. D., Single-channel observations on the mu-opioid receptor.Biophys. J., 50, 759–760 (1986).
Yuge, O., Matsumoto, M., Kitahara, L. M., Collins, J. G. and Senami, M., Direct opioid application to peripheral nerves does not alter compound action potentials.Anesth. Analg., 64, 667–671 (1985).
Zukin, S. R., Differing stereospecificities distinguish opiate receptor subtypes.Life Sci., 31, 1307–1310 (1982).
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Lee, J.H., Frank, G.B. Effects of opioid pure agonists on the excitibility of frog sciatic nerve fibers. Arch. Pharm. Res. 16, 83–88 (1993). https://doi.org/10.1007/BF03036851
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DOI: https://doi.org/10.1007/BF03036851