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. 1982 May;76(1):37–43. doi: 10.1111/j.1476-5381.1982.tb09188.x

Further analysis of inhibitory effects of propranolol and local anaesthetics on the calcium current in Helix neurones.

N Akaike, H Ito, K Nishi, Y Oyama
PMCID: PMC2068752  PMID: 7082906

Abstract

1 The effects of propranolol and local anaesthetics on Ca2+ current (Ica), individually separated from other ionic currents, in Helix neurones were studied under voltage clamp, using a suction pipette technique. 2 Increases in external Ca2+ concentrations overcame the inhibitory action of propranolol on Ica. Double reciprocal plots for peak Ica versus external Ca2+ concentrations in the presence or absence of propranolol did not intersect at the ordinate. 3 Internal application of propranolol (10-4M) inhibited Ica to about 40-60% of the control in a time-dependent manner. 4 Lignocaine and procaine at concentrations of 10-3-10-2 M inhibited Ica without shifting the threshold in the I-V relationships. Internal application of lignocaine (10-3-10-2M) also inhibited Ica: the ratio of depression of the Ica was almost equivalent to that of the agent applied externally. 5 The results provide evidence that propranolol inhibits Ica in the noncompetitive manner with Ca2+ at the cell membrane, and suggest that the agents may occupy the receptor site in the Ca2+-channel somewhere between the outer surface and inner phase of the membrane.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Akaike N., Brown A. M., Nishi K., Tsuda Y. Actions of verapamil, diltiazem and other divalent cations on the calcium-current of Helix neurones. Br J Pharmacol. 1981 Sep;74(1):87–95. doi: 10.1111/j.1476-5381.1981.tb09958.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Akaike N., Lee K. S., Brown A. M. The calcium current of Helix neuron. J Gen Physiol. 1978 May;71(5):509–531. doi: 10.1085/jgp.71.5.509. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Akaike N., Nishi K., Oyama Y. Inhibitory effects of propranolol on the calcium current of Helix neurones. Br J Pharmacol. 1981 Jun;73(2):431–434. doi: 10.1111/j.1476-5381.1981.tb10439.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Bigger J. T., Jr, Mandel W. J. Effect of lidocaine on the electrophysiological properties of ventricular muscle and purkinje fibers. J Clin Invest. 1970 Jan;49(1):63–77. doi: 10.1172/JCI106224. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Blaustein M. P., Goldman D. E. Competitive action of calcium and procaine on lobster axon. A study of the mechanism of action of certain local anesthetics. J Gen Physiol. 1966 May;49(5):1043–1063. doi: 10.1085/jgp.49.5.1043. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Davis L. D., Temte J. V. Electrophysiological actions of lidocaine on canine ventricular muscle and Purkinje fibers. Circ Res. 1969 May;24(5):639–655. doi: 10.1161/01.res.24.5.639. [DOI] [PubMed] [Google Scholar]
  7. FLECKENSTEIN A. DIE BEDEUTUNG DER ENERGIEREICHEN PHOSPHOSPHATE FUER KONTRAKTILITAET UND TONUS DES MYOKARDS. Verh Dtsch Ges Inn Med. 1964;70:81–99. [PubMed] [Google Scholar]
  8. Feinstein M. B., Paimre M. Mode of anticholinergic action of local anaesthetics. Nature. 1967 Apr 8;214(5084):151–153. doi: 10.1038/214151a0. [DOI] [PubMed] [Google Scholar]
  9. Hagiwara S., Takahashi K. Surface density of calcium ions and calcium spikes in the barnacle muscle fiber membrane. J Gen Physiol. 1967 Jan;50(3):583–601. doi: 10.1085/jgp.50.3.583. [DOI] [PMC free article] [PubMed] [Google Scholar]
  10. Hashimoto K., Satoh H., Imai S. Effects of etafenone and antiarrhythmic drugs on Na and Ca channels of guinea pig atrial muscle. J Cardiovasc Pharmacol. 1979 Sep-Oct;1(5):561–570. doi: 10.1097/00005344-197909000-00008. [DOI] [PubMed] [Google Scholar]
  11. Hille B. Local anesthetics: hydrophilic and hydrophobic pathways for the drug-receptor reaction. J Gen Physiol. 1977 Apr;69(4):497–515. doi: 10.1085/jgp.69.4.497. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Kass R. S., Tsien R. W. Multiple effects of calcium antagonists on plateau currents in cardiac Purkinje fibers. J Gen Physiol. 1975 Aug;66(2):169–192. doi: 10.1085/jgp.66.2.169. [DOI] [PMC free article] [PubMed] [Google Scholar]
  13. Lee K. S., Akaike N., Brown A. M. Properties of internally perfused, voltage-clamped, isolated nerve cell bodies. J Gen Physiol. 1978 May;71(5):489–507. doi: 10.1085/jgp.71.5.489. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Nakajima H., Hoshiyama M., Yamashita K., Kiyomoto A. Effect of diltiazem on electrical and mechanical activity of isolated cardiac ventricular muscle of guinea pig. Jpn J Pharmacol. 1975 Aug;25(4):383–392. doi: 10.1254/jjp.25.383. [DOI] [PubMed] [Google Scholar]
  15. Narahashi T., Moore J. W., Poston R. N. Anesthetic blocking of nerve membrane conductances by internal and external applications. J Neurobiol. 1969;1(1):3–22. doi: 10.1002/neu.480010103. [DOI] [PubMed] [Google Scholar]
  16. Parmley W. W., Braunwald E. Comparative myocardial depressant and anti-arrhythmic properties of d-propranolol, dl-propranolol and quinidine. J Pharmacol Exp Ther. 1967 Oct;158(1):11–21. [PubMed] [Google Scholar]
  17. Ritchie J. M. A pharmacological approach to the structure of sodium channels in myelinated axons. Annu Rev Neurosci. 1979;2:341–362. doi: 10.1146/annurev.ne.02.030179.002013. [DOI] [PubMed] [Google Scholar]
  18. Ritchie J. M. Mechanism of action of local anaesthetic agents and biotoxins. Br J Anaesth. 1975 Feb;47 Suppl:191–198. [PubMed] [Google Scholar]
  19. SHANES A. M., FREYGANG W. H., GRUNDFEST H., AMATNIEK E. Anesthetic and calcium action in the voltage-clamped squid giant axon. J Gen Physiol. 1959 Mar 20;42(4):793–802. doi: 10.1085/jgp.42.4.793. [DOI] [PMC free article] [PubMed] [Google Scholar]
  20. Sakanashi M., Nishi K. Relaxation of isolated dog coronary artery induced by propranolol. Eur J Pharmacol. 1981 Mar 5;70(1):83–85. doi: 10.1016/0014-2999(81)90436-2. [DOI] [PubMed] [Google Scholar]
  21. TAYLOR R. E. Effect of procaine on electrical properties of squid axon membrane. Am J Physiol. 1959 May;196(5):1071–1078. doi: 10.1152/ajplegacy.1959.196.5.1071. [DOI] [PubMed] [Google Scholar]

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