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PMID: 7670736 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

Quinidine-induced open channel block of K+ current in rat ventricle.

British journal of pharmacology ·Vol. 115 ·No. 2 ·1995-05-00 ·Pages 335-43

Clark RB, Sanchez-Chapula J, Salinas-Stefanon E, Duff HJ, Giles WR

Abstract

1. The effects of quinidine on calcium-independent outward K+ currents in rat ventricular myocytes were studied using whole-cell patch clamp techniques. 2. Quinidine sulphate (6 microM) significantly prolonged repolarization of the ventricular action potential. This effect was larger during early repolarization (25% level) than at later times (90% level). 3. Quinidine reduced the amplitude of a transient outward current, and accelerated its rate of decay by approximately 4 fold at membrane potentials between 0 to +50 mV. Quinidine also reduced the amplitude of a slowly inactivating, tetraethylammonium-sensitive 'pedestal' component of the outward current. 4. The quinidine-induced block of the transient outward current was dependent on time and membrane potential. Maximal block occurred with depolarizations of about 100 ms duration, and longer depolarizations (up to 1.5 s) produced little additional block. The membrane potential dependence of quinidine-induced block was very similar to the membrane potential dependence of activation of the transient outward current. The membrane potential dependence of steady-state inactivation of the transient outward current was not significantly affected by quinidine. 5. These results show that quinidine blocks outward K+ currents in rat ventricular cells. The time and potential dependence of this block suggests that quinidine blocks the transient outward K+ current by acting primarily on the open state of these channels.

MeSH Terms
Action Potentials/drug effects Animals Electrophysiology Heart Ventricles/cytology,drug effects,metabolism Patch-Clamp Techniques Potassium Channel Blockers Potassium Channels/drug effects Quinidine/pharmacology Rats Tetraethylammonium Tetraethylammonium Compounds/pharmacology
Chemicals
Potassium Channel Blockers Potassium Channels Tetraethylammonium Compounds Tetraethylammonium Quinidine
Authors & Affiliations
5 authors, click to expand affiliations / ORCID
Clark R B
Department of Medical Physiology, University of Calgary, School of Medicine, Alberta, Canada.
Sanchez-Chapula J
Salinas-Stefanon E
Duff H J
Giles W R
References (38)
38 references, click to expand
  1. Interaction of tetraethylammonium ion derivatives with the potassium channels of giant axons.
    J Gen Physiol. 1971 Oct;58(4):413-37 PMID: 5112659
  2. Characterization of two distinct depolarization-activated K+ currents in isolated adult rat ventricular myocytes.
    J Gen Physiol. 1991 May;97(5):973-1011 PMID: 1865177
  3. Local anesthetics: hydrophilic and hydrophobic pathways for the drug-receptor reaction.
    J Gen Physiol. 1977 Apr;69(4):497-515 PMID: 300786
  4. Time- and voltage-dependent interactions of antiarrhythmic drugs with cardiac sodium channels.
    Biochim Biophys Acta. 1977 Nov 14;472(3-4):373-98 PMID: 334262
  5. Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches.
    Pflugers Arch. 1981 Aug;391(2):85-100 PMID: 6270629
  6. Mechanisms of action of lidocaine and quinidine on action potential duration in rabbit cardiac Purkinje fibers. An effect on steady state sodium currents?
    Circ Res. 1982 Jan;50(1):17-27 PMID: 6274542
  7. Antiarrhythmic agents: the modulated receptor mechanism of action of sodium and calcium channel-blocking drugs.
    Annu Rev Pharmacol Toxicol. 1984;24:387-423 PMID: 6203481
  8. Action of quinidine on ionic currents of molluscan pacemaker neurons.
    J Gen Physiol. 1984 Jun;83(6):919-40 PMID: 6330283
  9. Control of cardiac arrhythmias by selective lengthening of repolarization: theoretic considerations and clinical observations.
    Am Heart J. 1985 Feb;109(2):421-30 PMID: 2578243
  10. Evidence for a specific receptor site for lidocaine, quinidine, and bupivacaine associated with cardiac sodium channels in guinea pig ventricular myocardium.
    Circ Res. 1985 Apr;56(4):496-506 PMID: 2579747
  11. Action potential prolongation and induction of abnormal automaticity by low quinidine concentrations in canine Purkinje fibers. Relationship to potassium and cycle length.
    Circ Res. 1985 Jun;56(6):857-67 PMID: 4006095
  12. Effects of quinidine on plateau currents of guinea-pig ventricular myocytes.
    J Mol Cell Cardiol. 1986 Oct;18(10):1097-106 PMID: 3783725
  13. Quinidine-induced inhibition of transient outward current in cardiac muscle.
    Am J Physiol. 1987 Sep;253(3 Pt 2):H704-8 PMID: 2443024
  14. Effects of quinidine on action potentials and ionic currents in isolated canine ventricular myocytes.
    Circ Res. 1988 Feb;62(2):324-37 PMID: 2448058
  15. Quinidine delays IK activation in guinea pig ventricular myocytes.
    Circ Res. 1988 May;62(5):1055-8 PMID: 2452034
  16. Time- and voltage-dependent block of the delayed K+ current by quinidine in rabbit sinoatrial and atrioventricular nodes.
    J Pharmacol Exp Ther. 1989 Nov;251(2):756-63 PMID: 2810126
  17. Mechanisms of termination of reentrant atrial arrhythmias by class I and class III antiarrhythmic agents.
    Circ Res. 1989 Dec;65(6):1565-79 PMID: 2510953
  18. Class III antiarrhythmic agents have a lot of potential but a long way to go. Reduced effectiveness and dangers of reverse use dependence.
    Circulation. 1990 Feb;81(2):686-90 PMID: 2153477
  19. The Sicilian gambit. A new approach to the classification of antiarrhythmic drugs based on their actions on arrhythmogenic mechanisms. Task Force of the Working Group on Arrhythmias of the European Society of Cardiology.
    Circulation. 1991 Oct;84(4):1831-51 PMID: 1717173
  20. Quinidine-induced inhibition of the fast transient outward K+ current in rat melanotrophs.
    Br J Pharmacol. 1991 Jul;103(3):1807-13 PMID: 1933143
  21. Time-, voltage-, and state-dependent block by quinidine of a cloned human cardiac potassium channel.
    Mol Pharmacol. 1992 Feb;41(2):322-30 PMID: 1538710
  22. Therapeutic potential of modulating potassium currents in the diseased myocardium.
    FASEB J. 1992 Aug;6(11):2952-60 PMID: 1386585
  23. Accelerating action of quinidine on the decay phase of transient outward current in dissociated hippocampal pyramidal neurons of rats.
    Jpn J Pharmacol. 1992 Feb;58(2):185-8 PMID: 1507524
  24. Molecular biology of voltage-dependent potassium channels.
    Physiol Rev. 1992 Oct;72(4 Suppl):S69-88 PMID: 1438587
  25. Differential effects of the new class III antiarrhythmic agents almokalant, E-4031 and D-sotalol, and of quinidine, on delayed rectifier currents in guinea pig ventricular myocytes.
    Cardiovasc Res. 1992 Nov;26(11):1145-52 PMID: 1291093
  26. Block of transient outward-type cloned cardiac K+ channel currents by quinidine.
    Circ Res. 1993 Aug;73(2):351-9 PMID: 8330377
  27. Heterogeneity of action potential waveforms and potassium currents in rat ventricle.
    Cardiovasc Res. 1993 Oct;27(10):1795-9 PMID: 8275526
  28. K+ channel blocking actions of flecainide compared with those of propafenone and quinidine in adult rat ventricular myocytes.
    J Pharmacol Exp Ther. 1994 Apr;269(1):66-74 PMID: 8169853
  29. Voltage-dependent gating of Shaker A-type potassium channels in Drosophila muscle.
    J Gen Physiol. 1990 Jan;95(1):29-60 PMID: 2299331
  30. Evidence for the formation of heteromultimeric potassium channels in Xenopus oocytes.
    Nature. 1990 Jun 7;345(6275):530-4 PMID: 2112229
  31. Molecular cloning and functional expression of a potassium channel cDNA isolated from a rat cardiac library.
    FEBS Lett. 1990 Jul 30;268(1):63-8 PMID: 2384173
  32. Two components of cardiac delayed rectifier K+ current. Differential sensitivity to block by class III antiarrhythmic agents.
    J Gen Physiol. 1990 Jul;96(1):195-215 PMID: 2170562
  33. Quinidine blocks adenosine 5'-triphosphate-sensitive potassium channels in heart.
    Am J Physiol. 1990 Nov;259(5 Pt 2):H1609-12 PMID: 2240258
  34. Channel specificity in antiarrhythmic drug action. Mechanism of potassium channel block and its role in suppressing and aggravating cardiac arrhythmias.
    Circulation. 1990 Dec;82(6):2235-42 PMID: 2242545
  35. Single inward rectifier potassium channels in guinea pig ventricular myocytes. Effects of quinidine.
    Biophys J. 1991 Jan;59(1):150-61 PMID: 2015380
  36. Antiarrhythmic drug classifications. A critical appraisal of their history, present status, and clinical relevance.
    Drugs. 1991 May;41(5):672-701 PMID: 1712704
  37. Suppression of time-dependent outward current in guinea pig ventricular myocytes. Actions of quinidine and amiodarone.
    Circ Res. 1991 Aug;69(2):519-29 PMID: 1860189
  38. Ionic blockage of sodium channels in nerve.
    J Gen Physiol. 1973 Jun;61(6):687-708 PMID: 4541078
Article Info
Journal
British journal of pharmacology
Abbr.
Br J Pharmacol
ISSN
0007-1188
Published
1995-05-00
Pages
335-43
Language
English
Region
England
NLM ID
7502536
PMCID
PMC1908313
Subset
IM
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