Class i antiarrhythmic drugs inhibit human cardiac two-pore-domain K + (K2P) channels

European Journal of Pharmacology

Volumn 721, Issue 1-3, 2013, Pages 237-248

  Schmidt, Constanze ^a   Wiedmann, Felix ^a   Schweizer, Patrick A ^a   Becker, Rüdiger ^a   Katus, Hugo A ^a   Thomas, Dierk ^a  

^a UNIVERSITY HOSPITAL HEIDELBERG   (Germany)

Author keywords

Ajmaline; Antiarrhythmic drug; Cardiac arrhythmia; Cellular excitability; K2P channel; Membrane potential; Mexiletine; Propafenone

Indexed keywords

AJMALINE; ANTIARRHYTHMIC AGENT; MEXILETINE; POTASSIUM CHANNEL K2P 2.1; POTASSIUM CHANNEL K2P 3.1; PROPAFENONE; TANDEM PORE DOMAIN POTASSIUM CHANNEL; UNCLASSIFIED DRUG;

ANIMAL CELL; ANTIARRHYTHMIC ACTIVITY; ARTICLE; CELL MEMBRANE DEPOLARIZATION; CHO CELL; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG CLASSIFICATION; DRUG SENSITIVITY; DRUG TARGETING; HEART ATRIUM FIBRILLATION; IC 50; MAMMAL CELL; MEMBRANE STEADY POTENTIAL; NONHUMAN; OOCYTE; PRIORITY JOURNAL; WHOLE CELL PATCH CLAMP; XENOPUS;

AJMALINE; ANTIARRHYTHMIC DRUG; CARDIAC ARRHYTHMIA; CELLULAR EXCITABILITY; K(2P) CHANNEL; MEMBRANE POTENTIAL; MEXILETINE; PROPAFENONE;

ACTION POTENTIALS; ANIMALS; ANTI-ARRHYTHMIA AGENTS; CHO CELLS; CRICETINAE; CRICETULUS; HUMANS; MEXILETINE; MYOCARDIUM; OOCYTES; POTASSIUM CHANNEL BLOCKERS; POTASSIUM CHANNELS, TANDEM PORE DOMAIN; PROPAFENONE; XENOPUS LAEVIS;

EID: 84890116891     PISSN: 00142999     EISSN: 18790712     Source Type: Journal    
DOI: 10.1016/j.ejphar.2013.09.029     Document Type: Article

References (60)

1. + channels Molecular Interventions 4 2003 205 219
2. M.C. Bigot, D. Debruyne, L. Bonnefoy, G. Grollier, M. Moulin, and J.C. Potier Serum digoxin levels related to plasma propafenone levels during concomitant treatment Journal of Clinical Pharmacology 31 1991 521 526
3. S.A. Cahill, and G.J. Gross Propafenone and its metabolites preferentially inhibit IKr in rabbit ventricular myocytes Journal of Pharmacology and Experimental Therapeutics 308 2004 59 65 (Pubitemid 38090700)
4. W.M. Cai, J. Xu, B. Chen, F.M. Zhang, Y.Z. Huang, and Y.D. Zhang Effect of CYP2D6â10 genotype on propafenone pharmacodynamics in Chinese patients with ventricular arrhythmia Acta Pharmacologica Sinica 23 2002 1040 1044 (Pubitemid 35285191)
5. A.J. Camm, G.Y. Lip, R. De Caterina, I. Savelieva, D. Atar, S.H. Hohnloser, G. Hindricks, P. Kirchhof ESC Committee for Practice Guidelines (CPG) J.J. Bax, H. Baumgartner, C. Ceconi, V. Dean, C. Deaton, R. Fagard, C. Funck-Brentano, D. Hasdai, A. Hoes, P. Kirchhof, J. Knuuti, P. Kolh, T. McDonagh, C. Moulin, B.A. Popescu, Z. Reiner, U. Sechtem, P.A. Sirnes, M. Tendera, A. Torbicki, A. Vahanian, S. Windecker Document Reviewers P. Vardas, N. Al-Attar, O. Alfieri, A. Angelini, C. Blömstrom-Lundqvist, P. Colonna, J. De Sutter, S. Ernst, A. Goette, B. Gorenek, R. Hatala, H. Heidbüchel, M. Heldal, S.D. Kristensen, P. Kolh, J.Y. Le Heuzey, H. Mavrakis, L. Mont, P.P. Filardi, P. Ponikowski, B. Prendergast, F.H. Rutten, U. Schotten, I.C. Van Gelder, and F.W. Verheugt 2012 focused update of the ESC Guidelines for the management of atrial fibrillation: an update of the 2010 ESC Guidelines for the management of atrial fibrillation. Developed with the special contribution of the European Heart Rhythm Association European Heart Journal 33 2012 2719 2747
6. D. Darbar, and D.M. Roden Pharmacogenetics of antiarrhythmic therapy Expert Opinion on Pharmacotherapy 7 2006 1583 1590 (Pubitemid 44209602)
7. N. Decher, K. Wemhöner, S. Rinné, M.F. Netter, M. Zuzarte, M.I. Aller, S.G. Kaufmann, X.T. Li, S.G. Meuth, J. Daut, F.B. Sachse, and S.K. Maier Knock-out of the potassium channel TASK-1 leads to a prolonged QT interval and a disturbed QRS complex Cellular Physiology and Biochemistry 28 2011 77 86
8. C. Delgado, J. Tamargo, D. Henzel, and P. Lorente Effects of propafenone on calcium current in guinea-pig ventricular myocytes British Journal of Pharmacology 108 1993 721 727 (Pubitemid 23067943)
9. B.C. Donner, M. Schullenberg, N. Geduldig, A. Hüning, J. Mersmann, K. Zacharowski, A. Kovacevic, U. Decking, M.I. Aller, and K.G. Schmidt Functional role of TASK-1 in the heart: studies in TASK-1 deficient mice show prolonged cardiac repolarization and reduced heart variability Basic Research in Cardiology 106 2011 75 87
10. D. Duan, B. Fermini, and S. Nattel Potassium channel blocking properties of propafenone in rabbit atrial myocytes Journal of Pharmacology and Experimental Therapeutics 264 1993 1113 1123 (Pubitemid 23318601)
11. F. Duprat, F. Lesage, M. Fink, R. Reyes, C. Heurteaux, and M. Lazdunski TASK, a human background K+ channel to sense external pH variations near physiological pH EMBO Journal 16 1997 5464 5471 (Pubitemid 27380153)
12. T. Edrich, S.Y. Wang, and G.K. Wang State-dependent block of human cardiac hNav1.5 sodium channels by propafenone Journal of Membrane Biology 207 2005 35 43 (Pubitemid 43208511)
13. 2P) potassium leak channels by the tyrosine kinase inhibitor genistein British Journal of Pharmacology 154 2008 1680 1690
14. 2P3.1 (TASK-1). potassium leak channel is a molecular target for the class III antiarrhythmic drug amiodarone Naunyn-Schmiedeberg's Archives of Pharmacology 381 2010 261 270
15. + channels Biochimica et Biophysica Acta 1818 2012 33 41
16. G.J. Gross, and N.A. Castle Propafenone inhibition of human atrial myocyte repolarizing currents Journal of Molecular and Cellular Cardiology 30 1998 783 793 (Pubitemid 28190722)
17. J.C. Hancox, and J.S. Mitcheson Inhibition of l-type calcium current by propafenone in single myocytes isolated from the rabbit atrioventricular node British Journal of Pharmacology 121 1997 7 14 (Pubitemid 27192782)
18. N. Hanioka, Y. Okumura, Y. Saito, H. Hichiya, A. Soyama, K. Saito, K. Ueno, J. Sawada, and S. Narimatsu Catalytic roles of CYP2D6.10 and CYP2D6.36 enzymes in mexiletine metabolism: in vitro functional analysis of recombinant proteins expressed in Saccharomyces cerevisiae Biochemical Pharmacology 71 2006 1386 1395
19. + channel and drug-induced prolongation of the QRS complex British Journal of Pharmacology 164 2011 260 273
20. C. Kiesecker, E. Zitron, S. Lück, R. Bloehs, E.P. Scholz, S. Kathöfer, D. Thomas, V.A. Kreye, H.A. Katus, W. Schoels, C.A. Karle, and J. Kiehn Class Ia anti-arrhythmic drug ajmaline blocks HERG potassium channels: mode of action Naunyn-Schmiedeberg's Archives of Pharmacology 370 2004 423 435 (Pubitemid 40104755)
21. C.H. Kindler, C.S. Yost, and A.T. Gray Local anesthetic inhibition of baseline potassium channels with two pores in tandem Anesthesiology 90 1999 1092 1102 (Pubitemid 29159768)
22. + channel β subunits Life Sciences 91 2012 377 383
23. D. Leonoudakis, A.T. Gray, B.D. Winegar, C.H. Kindler, M. Harada, D.M. Taylor, R.A. Chavez, J.R. Forsayeth, and C.S. Yost An open rectifier potassium channel with two pore domains in tandem cloned from rat cerebellum Journal of Neuroscience 18 1998 868 877 (Pubitemid 28112909)
24. S.H. Limberg, M.F. Netter, C. Rolfes, S. Rinné, G. Schlichthörl, M. Zuzarte, T. Vassiliou, R. Moosdorf, H. Wulf, J. Daut, F.B. Sachse, and N. Decher TASK-1 channels may modulate action potential duration of human atrial cardiomyocytes Cellular Physiology and Biochemistry 28 2011 613 624
25. C.M.B. Lopes, P.G. Gallagher, M.E. Buck, M.H. Butler, and S.A.N. Goldstein Proton block and voltage-gating are potassium-dependent in the cardiac leak channel Kcnk3 Journal of Biological Chemistry 275 2000 16969 16978 (Pubitemid 30398937)
26. Xian Tao Li, V. Dyachenko, M. Zuzarte, C. Putzke, R. Preisig-Müller, G. Isenberg, and J. Daut The stretch-activated potassium channel TREK-1 in rat cardiac ventricular muscle Cardiovascular Research 69 2006 86 97 (Pubitemid 41814814)
27. J.S. Mitcheson, and J.C. Hancox Modulation by mexiletine of action potentials, l-type Ca current and delayed rectifier K current recorded from isolated rabbit atrioventricular nodal myocytes Pflügers Archives 434 1997 855 858 (Pubitemid 28066438)
28. T.K. Nayak, S. Harinath, S. Nama, K. Somasundaram, and S.K. Sikdar Inhibition of human two-pore domain K+ channel TREK1 by local anesthetic lidocaine: negative cooperativity and half-of-sites saturation kinetics Molecular Pharmacology 76 2009 903 917
29. J. Nicholas, D.M. Boyle, C.D. Kinney, K. Salathia, and R.G. Shanks Plasma concentrations and acceptability of mexiletine given by intramuscular injection in patients admitted to a coronary care unit Journal of Cardiovascular Pharmacology 8 1986 21 28 (Pubitemid 16149387)
30. G.E. O'Hara, F. Philippon, M. Gilbert, J. Champagne, V. Michaud, L. Charbonneau, G. Pruneau, B.A. Hamelin, P. Geelen, and J. Turgeon Combined administration of quinidine and propafenone for atrial fibrillation: the CAQ-PAF study Journal of Clinical Pharmacology 52 2012 171 179
31. S. Obers, I. Staudacher, E. Ficker, A. Dennis, R. Koschny, H. Erdal, R. Bloehs, J. Kisselbach, C.A. Karle, P.A. Schweizer, H.A. Katus, and D. Thomas Multiple mechanisms of hERG liability: K+ current inhibition, disruption of protein trafficking, and apoptosis induced by amoxapine Naunyn-Schmiedeberg's Archives of Pharmacology 381 2010 385 400
32. M. Otani, T. Fukuda, M. Naohara, H. Maune, C. Senda, I. Yamamoto, and J. Azuma Impact of CYP2D6â10 on mexiletine pharmacokinetics in healthy adult volunteers European Journal of Clinical Pharmacology 59 2003 395 399 (Pubitemid 37214945)
33. A. Pacifico, and P.D. Henry Class I or class III agents for atrial fibrillation: are asking the right question? Pacing and Clinical Electrophysiology 26 2003 1613 1619 (Pubitemid 36840930)
34. + channels Trends in Neurosciences 24 2001 339 346 (Pubitemid 32455435)
35. A.A. Paul, H.J. Witchel, and J.C. Hancox Inhibition of the current of heterologously expressed HERG potassium channels by flecainide and comparison with quinidine, propafenone and lignocaine British Journal of Pharmacology 136 2002 717 729 (Pubitemid 34785714)
36. S. Petric, L. Clasen, C. van Wessel, N. Geduldig, Z. Ding, M. Schullenberg, J. Mersmann, K. Zacharowski, M.I. Aller, K.G. Schmidt, and B.C. Donner In vivo electrophysiological characterization of TASK-1 deficient mice Cellular Physiology and Biochemistry 30 2012 523 537
37. C. Putzke, K. Wemhöner, F.B. Sachse, S. Rinné, G. Schlichthörl, X.T. Li, L. Jaé, I. Eckhardt, E. Wischmeyer, H. Wulf, R. Preisig-Müller, J. Daut, and N. Decher The acid-sensitive potassium channel TASK-1 in rat cardiac muscle Cardiovascular Research 75 2007 59 68 (Pubitemid 46873507)
38. + channels British Journal of Pharmacology 166 2012 764 773
39. U. Ravens Novel pharmacological approaches for antiarrhythmic therapy Naunyn-Schmiedeberg's Archives of Pharmacology 381 2010 187 193
40. S. Rolf, W. Haverkamp, M. Borggrefe, U. Musshoff, L. Eckardt, J. Mergenthaler, D.J. Snyders, O. Pongs, E.J. Speckmann, G. Breithardt, and M. Madeja Effects of antiarrhythmic drugs on cloned cardiac voltage-gated potassium channels expressed in Xenopus oocytes Naunyn-Schmiedeberg's Archives of Pharmacology 362 2000 22 31 (Pubitemid 30431632)
41. G. Sandoz, D. Douguet, F. Chatelain, M. Lazdunski, and F. Lesage Extracellular acidification exerts opposite actions on TREK1 and TREK2 potassium channels via a single conserved histidine residue Proceedings of the National Academy of Sciences of the United States of America 106 2009 14628 16433
42. C. Schmidt, J. Kisselbach, P.A. Schweizer, H.A. Katus, and D. Thomas The pathology and treatment of cardiac arrhythmias: Focus on atrial fibrillation Vascular Health and Risk Management 7 2011 193 202
43. 2P) channels Naunyn-Schmiedeberg's Archives of Pharmacology 385 2012 1003 1016
44. A. Seki, N. Hagiwara, and H. Kasanuki Effects of propafenone on K currents in human atrial myocytes British Journal of Pharmacology 126 1999 1153 1162 (Pubitemid 29123750)
45. C. Senda, Y. Yamaura, K. Kobayashi, H. Fujii, H. Minami, Y. Sasaki, T. Igarashi, and K. Chiba Influence of the CYP2D6â10 allele on the metabolism of mexiletine by human liver microsomes British Journal of Clinical Pharmacology 52 2001 100 103 (Pubitemid 32862776)
46. 2P3.1) K+ current inhibition by endothelin-1 is mediated by Rho kinase-dependent channel phosphorylation British Journal of Pharmacology 165 2012 1467 1475
47. 2P10.1 K+ channels Journal of Physiology 589 2011 3709 3720
48. 2P3.1 (TASK1) K+ leak channels British Journal of Pharmacology 163 2011 1099 1110
49. I. Staudacher, L. Wang, X. Wan, S. Obers, W. Wenzel, F. Tristram, R. Koschny, K. Staudacher, J. Kisselbach, P. Koelsch, P.A. Schweizer, H.A. Katus, E. Ficker, and D. Thomas hERG K+ channel-associated cardiac effects of the antidepressant drug desipramine Naunyn-Schmiedeberg's Archives of Pharmacology 383 2011 119 139
50. A. Tamura, T. Ogura, H. Uemura, Y. Reien, T. Kishimoto, T. Nagai, I. Komuro, M. Miyazaki, and H. Nakaya Effects of antiarrhythmic drugs on the hyperpolarization-activated cyclic nucleotide-gated channel current Journal of Pharmacological Sciences 110 2009 150 159
51. T. Tanabe, H. Yoshikawa, H. Furuya, and Y. Goto Therapeutic effectiveness and plasma levels of single or combination use of class I antiarrhythmic agents for ventricular arrhythmias Japanese Circulation Society 52 1988 298 305
52. 2P2.1 potassium channels permeable to sodium Neuron 58 2008 859 870 (Pubitemid 351842748)
53. D. Thomas, G. Wendt-Nordahl, K. Röckl, E. Ficker, A.M. Brown, and J. Kiehn High-affinity blockade of human ether-a-go-go-related gene human cardiac potassium channels by the novel antiarrhythmic drug BRL-32872 Journal of Pharmacology and Experimental Therapeutics 297 2001 753 761 (Pubitemid 32378009)
54. D. Thomas, A.B. Wimmer, K. Wu, B.C. Hammerling, E.K. Ficker, Y.A. Kuryshev, J. Kiehn, H.A. Katus, W. Schoels, and C.A. Karle Inhibition of human ether-a-go-go-related gene potassium channels by alpha 1-adrenoceptor antagonists prazosin, doxazosin, and terazosin Naunyn-Schmiedeberg's Archives of Pharmacology 369 2004 462 472 (Pubitemid 38669965)
55. N. Voigt, N. Rozmaritsa, A. Trausch, T. Zimniak, T. Christ, E. Wettwer, K. Matschke, D. Dobrev, and U. Ravens Inhibition of IK,ACh current may contribute to clinical efficacy of class I and class III antiarrhythmic drugs in patients with atrial fibrillation Naunyn-Schmiedeberg's Archives of Pharmacology 381 2010 251 259
56. M. Volz, V. Mitrovic, J. Thiemer, and M. Schlepper Steady-state plasma kinetics of slow-release propafenone, its two isomers and its main metabolites Arzneimittelforschung 45 1995 246 249
57. L.S. Wann, A.B. Curtis, C.T. January, K.A. Ellenbogen, J.E. Lowe, N.A. Estes 3rd, R.L. Page, M.D. Ezekowitz, D.J. Slotwiner, W.M. Jackman, W.G. Stevenson, C.M. Tracy 2011 Writing Group Members V. Fuster, L.E. Rydén, D.S. Cannom, J.Y. Le Heuzey, H.J. Crijns, J.E. Lowe, A.B. Curtis, S. Olsson, K.A. Ellenbogen, E.N. Prystowsky, J.L. Halperin, J.L. Tamargo, G.N. Kay, L. Wann 2006 Writing Committee Members A.K. Jacobs, J.L. Anderson, N. Albert, J.S. Hochman, C.E. Buller, F.G. Kushner, M.A. Creager, E.M. Ohman, S.M. Ettinger, W.G. Stevenson, R.A. Guyton, L.G. Tarkington, J.L. Halperin, C.W. Yancy ACCF/AHA Task Force Members 2011 ACCF/AHA/HRS focused update on the management of patients with atrial fibrillation (updating the 2006 guideline): a report of the American College of Cardiology Foundation/American Heart Association Task Force on Practice Guidelines Circulation 123 2011 104 123
58. A. Yatani, and N. Akaike Blockage of the sodium current in isolated single cells from rat ventricle with mexiletine and disopyramide Journal of Molecular and Cellular Cardiology 17 1985 467 476 (Pubitemid 15000343)
59. D.P. Zipes, A.J. Camm, M. Borggrefe, A.E. Buxton, B. Chaitman, M. Fromer, G. Gregoratos, G. Klein, A.J. Moss, R.J. Myerburg, S.G. Priori, M.A. Quinones, D.M. Roden, M.J. Silka, C. Tracy, J.J. Blanc, A. Budaj, V. Dean, J.W. Deckers, C. Despres, K. Dickstein, J. Lekakis, K. McGregor, M. Metra, J. Morais, A. Osterspey, J.L. Tamargo, J.L. Zamorano, S.C. Smith Jr, A.K. Jacobs, C.D. Adams, E.M. Antman, J.L. Anderson, S.A. Hunt, J.L. Halperin, R. Nishimura, J.P. Ornato, R.L. Page, B. Riegel American College of Cardiology/American Heart Association Task Force; European Society of Cardiology Committee for Practice Guidelines; European Heart Rhythm Association and the Heart Rhythm Society ACC/AHA/ESC 2006 guidelines for management of patients with ventricular arrhythmias and the prevention of sudden cardiac death - executive summary: a report of the American College of Cardiology/American Heart Association Task Force and the European Society of Cardiology Committee for Practice Guidelines (Writing Committee to Develop Guidelines for Management of Patients with Ventricular Arrhythmias and the Prevention of Sudden Cardiac Death) Developed in collaboration with the European Heart Rhythm Association and the Heart Rhythm Society European Heart Journal 27 2006 2099 2140
60. Zitron, E., Kiesecker, C., Scholz, E., Lck, S., Bloehs, R., Kathfer, S., Thomas, D., Kiehn, J., Kreye, V.A., Katus, H.A., Schoels, W., Karle, C.A., 2004. Inhibition of cardiac cardiac HERG potassium channels by the atypical antidepressant trazodone Naunyn-Schmiedeberg's Archives of Pharmacology 370,146-156. (Pubitemid 39222867)