Comparison of HERG channel blocking effects of various β-blockers - Implication for clinical strategy

British Journal of Pharmacology

Volumn 147, Issue 6, 2006, Pages 642-652

  Kawakami, Kazunobu ^a   Nagatomo, Toshihisa ^a   Abe, Haruhiko ^a   Kikuchi, Kan ^a   Takemasa, Hiroko ^a   Anson, Blake D ^b   Delisle, Brian P ^b   January, Craig T ^b   Nakashima, Yasuhide ^a  

^a UNIVERSITY OF OCCUPATIONAL AND ENVIRONMENTAL HEALTH   (Japan)

^b UNIVERSITY OF WISCONSIN SCHOOL OF MEDICINE AND PUBLIC HEALTH   (United States)

Author keywords

Blockers; Arrhythmia; Heart failure; HEK293 cells; Ion channels; K + channel; Long QT syndrome; Membrane currents

Indexed keywords

3 ISOPROPYLAMINO 1 (7 METHYL 4 INDANYLOXY) 2 BUTANOL; ATENOLOL; BETA ADRENERGIC RECEPTOR BLOCKING AGENT; CARVEDILOL; METOPROLOL; MUTANT PROTEIN; POTASSIUM CHANNEL HERG; PROPRANOLOL;

ANTIARRHYTHMIC ACTIVITY; ARTICLE; BINDING AFFINITY; CELL MEMBRANE POTENTIAL; CELL STRAIN HEK293; CLINICAL TRIAL; COMPARATIVE STUDY; CONCENTRATION RESPONSE; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DRUG BINDING; DRUG BINDING SITE; DRUG EFFECT; DRUG INDICATION; DRUG STRUCTURE; HEART ARRHYTHMIA; HUMAN; HUMAN CELL; IC 50; LONG QT SYNDROME; MEMBRANE CURRENT; MUTATION; NUCLEOTIDE SEQUENCE; PATCH CLAMP; PHARMACOLOGICAL BLOCKING; PRIORITY JOURNAL;

ADRENERGIC BETA-ANTAGONISTS; BINDING SITES; CARBAZOLES; CARDIOVASCULAR DISEASES; CELL LINE; DOSE-RESPONSE RELATIONSHIP, DRUG; ETHER-A-GO-GO POTASSIUM CHANNELS; HUMANS; LONG QT SYNDROME; MEMBRANE POTENTIALS; METOPROLOL; MUTATION; POTASSIUM CHANNEL BLOCKERS; PROPANOLAMINES; PROPRANOLOL; PROTEIN BINDING; TRANSFECTION;

EID: 33645105639     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1038/sj.bjp.0706508     Document Type: Article

References (43)

1. Kr potassium channels with HERG and is associated with cardiac arrhythmia. Cell, 97, 175-187.
2. CARMELIET, E. (1993). Mechanisms and control of repolarization. Eur. Heart J., 14 (Suppl H), 3-13.
3. 2+ current in rabbit ventricular myocytes. Eur. J. Pharmacol., 376, 189-201.
4. CUI, J., KAGAN, A., QIN, D., MATHEW, J., MELMAN, Y.F. & MCDONALD, T.V. (2001). Analysis of the cyclic nucleotide binding domain of the HERG potassium channel and interactions with KCNE2. J. Biol. Chem., 276, 17244-17251.
5. + channel by dual pathways. Curr. Biol., 10, 671-674.
6. CURRAN, M.E., SPLAWSKI, I., TIMOTHY, K.W., VINCENT, G.M., GREEN, E.D. & KEATING, M.T. (1995). A molecular basis for cardiac arrhythmia: HERG mutations cause long QT syndrome. Cell, 80, 795-803.
7. DOROSTKAR, P.C., ELDAR, M., BELHASSEN, B. & SCHEINMAN, M.M. (1999). Long-term follow-up of patients with long-QT syndrome treated with β-blockers and continuous pacing. Circulation, 100, 2431-2436.
8. DUPUIS, D.S., KLAERKE, D.A. & OLESEN, S.P. (2005). Effect of β-adrenoceptor blockers on human ether-a-go-go-related gene (HERG) potassium channels. Basic Clin. Pharmacol. Toxicol., 96, 123-130.
9. FARHANGI, V. & SANSONE, R.A. (2003). QTc prolongation due to propranolol overdose. Int. J. Psychiatry Med., 33, 201-202.
10. FRIEDERICH, P., SOLTH, A., SCHILLEMEIT, S. & ISBRANDT, D. (2004). Local anaesthetic sensitivities of cloned HERG channels from human heart: comparison with HERG/MiRP1 and HERG/MiRP1 T8A. Br. J. Anaesth., 92, 93-101.
11. + channels by vesnarinone. Mol. Pharmacol., 60, 244-253.
12. KARLE, C.A., KREYE, V.A., THOMAS, D., ROCKL, K., KATHOFER, S., ZHANG, W. & KIEHN, J. (2001). Antiarrhythmic drug carvedilol inhibits HERG potassium channels. Cardiovasc. Res., 49, 361-370.
13. 1- adrenoreceptor activation, via cAMP/protein kinase A-dependent pathways. Cardiovasc. Res., 53, 355-362.
14. + current by antifungal drug miconazole. Br. J. Pharmacol., 144, 840-848.
15. LINKER, N.J., COLONNA, P., KEKWICK, C.A., TILL, J., CAMM, A.J. & WARD, D.E. (1992). Assessment of QT dispersion in symptomatic patients with congenital long QT syndromes. Am. J. Cardiol., 69, 634-638.
16. MADEJA, M., MUSSHOFF, U. & SPECKMANN, E.J. (1997). Follicular tissues reduce drug effects on ion channels in oocytes of Xenopus laevis. Eur. J. Neurosci., 9, 599-604.
17. MCPHILLIPS, J.J., SCHWEMER, G.T., SCOTT, D.I., ZINNY, M. & PATTERSON, D. (1988). Effects of carvedilol on blood pressure in patients with mild to moderate hypertension. A dose response study. Drugs, 36 (Suppl 6), 82-91.
18. MILNES, J.T., CROCIANI, O., ARCANGELI, A., HANCOX, J.C. & WITCHEL, H.J. (2003). Blockade of HERG potassium currents by fluvoxamine: incomplete attenuation by S6 mutations at F656 or Y652. Br. J. Pharmacol., 139, 887-898.
19. MITCHESON, J.S., CHEN, J., LIN, M., CULBERSON, C. & SANGUINETTI, M.C. (2000). A structural basis for drug-induced long QT syndrome. Proc. Natl. Acad. Sci. U.S.A., 97, 12329-12333.
20. MOSS, A.J., ZAREBA, W., HALL, W.J., SCHWARTZ, P.J., CRAMPTON, R.S., BENHORIN, J., VINCENT, G.M., LOCATI, E.H., PRIORI, S.G., NAPOLITANO, C., MEDINA, A., ZHANG, L., ROBINSON, J.L., TIMOTHY, K., TOWBIN, J.A. & ANDREWS, M.L. (2000). Effectiveness and limitations of β-blocker therapy in congenital long-QT syndrome. Circulation, 101, 616-623.
21. NUMAGUCHI, H., MULLINS, F.M., JOHNSON Jr, J.P., JOHNS, D.C., PO, S.S., YANG, I.C., TOMASELLI, G.F. & BALSER, J.R. (2000). Probing the interaction between inactivation gating and Dd-sotalol block of HERG. Circ. Res., 87, 1012-1018.
22. PERRY, M., DE GROOT, M.J., HELLIWELL, R., LEISHMAN, D., TRISTANI-FIROUZI, M., SANGUINETTI, M.C. & MITCHESON, J.S. (2004). Structural determinants of HERG channel block by clofilium and ibutilide. Mol. Pharmacol., 66, 240-249.
23. POOLE-WILSON, P.A., SWEDBERG, K., CLELAND, J.G., DI LENARDA, A., HANRATH, P., KOMAJDA, M., LUBSEN, J., LUTIGER, B., METRA, M., REMME, W.J., TORP-PEDERSEN, C., SCHERHAG, A. & SKENE, A. (2003). Comparison of carvedilol and metoprolol on clinical outcomes in patients with chronic heart failure in the Carvedilol Or Metoprolol European Trial (COMET): randomised controlled trial. Lancet, 362, 7-13.
24. REDFERN, W.S., CARLSSON, L., DAVIS, A.S., LYNCH, W.G., MACKENZIE, I., PALETHORPE, S., SIEGL, P.K., STRANG, I., SULLIVAN, A.T., WALLIS, R., CAMM, A.J. & HAMMOND, T.G. (2003). Relationships between preclinical cardiac electrophysiology, clinical QT interval prolongation and torsade de pointes for a broad range of drugs: evidence for a provisional safety margin in drug development. Cardiovasc. Res., 58, 32-45.
25. REMME, W.J., CLELAND, J.G., DI LENARDA, A., HANRATH, P., LUTIGER, B., KOMAJDA, M., METRA, M., SCHERHAG, A., CHARLESWORTH, A. & TORP-PEDERSEN, C. (2004). Carvedilol better protects against vascular events than metoprolol in heart failure: results from COMET. J. Am. Coll. Cardiol., 43, A205-A206.
26. + channel blockade by the antiarrhythraic agent dronedarone: resistance to mutation of the S6 residues Y652 and F656. Biochem. Biophys. Res. Commun., 325, 883-891.
27. RODEN, D.M. (2004). Drug-induced prolongation of the QT interval. N. Engl. J. Med., 350, 1013-1022.
28. SANCHEZ-CHAPULA, J.A., FERRER, T., NAVARRO-POLANCO, R.A. & SANGUINETTI, M.C. (2003). Voltage-dependent profile of human ether-a-go-go-related gene channel block is influenced by a single residue in the S6 transmembrane domain. Mol. Pharmacol., 63, 1051-1058.
29. + current. Differential sensitivity to block by class III antiarrhythmic agents. J. Gen. Physiol., 96, 195-215.
30. SANGUINETTI, M.C., JIANG, C., CURRAN, M.E. & KEATING, M.T. (1995). A mechanistic link between an inherited and an acquired cardiac arrhythmia: HERG encodes the IKr potassium channel. Cell, 81, 299-307.
31. SCHERER, C.R., LERCHE, C., DECHER, N., DENNIS, A.T., MAIER, P., FICKER, E., BUSCH, A.E., WOLLNIK, B. & STEINMEYER, K. (2002). The antihistamine fexofenadine does not affect I(Kr) currents in a case report of drug-induced cardiac arrhythmia. Br. J. Pharmacol., 137, 892-900.
32. SCHOLZ, E.P., ZITRON, E., KIESECKER, C., LUECK, S., KATHOFER, S., THOMAS, D., WERETKA, S., PETH, S., KREYE, V.A., SCHOELS, W., KATUS, H.A., KIEHN, J. & KARLE, C.A. (2003). Drug binding to aromatic residues in the HERG channel pore cavity as possible explanation for acquired Long QT syndrome by antiparkinsonian drug budipine. Naunyn. Schmiedebergs. Arch. Pharmacol., 368, 404-414.
33. SCHWARTZ, P.J., PRIORI, S.G., SPAZZOLINI, C., MOSS, A.J., VINCENT, G.M., NAPOLITANO, C., DENJOY, I., GUICHENEY, P., BREITHARDT, G., KEATING, M.T., TOWBIN, J.A., BEGGS, A.H., BRINK, P., WILDE, A.A., TOIVONEN, L., ZAREBA, W., ROBINSON, J.L., TIMOTHY, K.W., CORFIELD, V., WATTANASIRICHAIGOON, D., CORBETT, C., HAVERKAMP, W., SCHULZE-BAHR, E., LEHMANN, M.H., SCHWARTZ, K., COUMEL, P. & BLOISE, R. (2001). Genotype-phenotype correlation in the long-QT syndrome: gene-specific triggers for life-threatening arrhythmias. Circulation, 103, 89-95.
34. SESTI, F., ABBOTT, G.W., WEI, J., MURRAY, K.T., SAKSENA, S., SCHWARTZ, P.J., PRIORI, S.G., RODEN, D.M., GEORGE Jr, A.L. & GOLDSTEIN, S.A. (2000). A common polymorphism associated with antibiotic-induced cardiac arrhythmia. Proc. Natl. Acad. Sci. U.S.A., 97, 10613-10618.
35. SHIMIZU, W. & ANTZELEVITCH, C. (1998). Cellular basis for the ECG features of the LQT1 form of the long-QT syndrome: effects of beta-adrenergic agonists and antagonists and sodium channel blockers on transmural dispersion of repolarization and torsade de pointes. Circulation, 98, 2314-2322.
36. SHIMIZU, W., TANABE, Y., AIBA, T., INAGAKI, M., KURITA, T., SUYAMA, K., NAGAYA, N., TAGUCHI, A., AIHARA, N., SUNAGAWA, K., NAKAMURA, K., OHE, T., TOWBIN, J.A., PRIORI, S.G. & KAMAKURA, S. (2002). Differential effects of beta-blockade on dispersion of repolarization in the absence and presence of sympathetic stimulation between the LQT1 and LQT2 forms of congenital long QT syndrome. J. Am. Coll. Cardiol., 39, 1984-1991.
37. SMITH, C. & TEITLER, M. (1999). Beta-blocker selectivity at cloned human beta 1- and beta 2-adrenergic receptors. Cardiovasc. Drugs Ther., 13, 123-126.
38. TAMARGO, J., CABALLERO, R., GOMEZ, R., VALENZUELA, C. & DELPON, E. (2004). Pharmacology of cardiac potassium channels. Cardiovasc. Res., 62, 9-33.
39. THOMAS, D., ZHANG, W., KARLE, C.A., KATHOFER, S., SCHOLS, W., KUBLER, W. & KIEHN, J. (1999). Deletion of protein kinase A phosphorylation sites in the HERG potassium channel inhibits activation shift by protein kinase A. J. Biol. Chem., 274, 27457-27462.
40. TRUDEAU, M.C., WARMKE, J.W., GANETZKY, B. & ROBERTSON, G.A. (1995). HERG, a human inward rectifier in the voltage-gated potassium channel family. Science, 269, 92-95.
41. VISKIN, S. (1999). Long QT syndromes and torsade de pointes. Lancet, 354, 1625-1633.
42. YAO, X., MCINTYRE, M.S., LANG, D.G., SONG, I.H., BECHERER, J.D. & HASHIM, M.A. (2005). Propranolol inhibits the human ether-a-go-go-related gene potassium channels. Eur. J. Pharmacol., 519, 208-211.
43. ZHOU, Z., GONG, Q., YE, B., FAN, Z., MAKIELSKI, J.C., ROBERTSON, G.A. & JANUARY, C.T. (1998). Properties of HERG channels stably expressed in HEK 293 cells studied at physiological temperature. Biophys. J., 74, 230-241.