Variability in the measurement of hERG potassium channel inhibition: Effects of temperature and stimulus pattern

Journal of Pharmacological and Toxicological Methods

Volumn 50, Issue 2, 2004, Pages 93-101

  Kirsch, Glenn E ^a   Trepakova, Elena S ^a   Brimecombe, Jessica C ^a   Sidach, Serguei S ^a   Erickson, Hope D ^a   Kochan, Mary C ^a   Shyjka, Lisa M ^a   Lacerda, Antonio E ^a   Brown, Arthur M ^b  

^a ChanTest Inc   (United States)

^b CASE WESTERN RESERVE UNIVERSITY   (United States)

Author keywords

Drug evaluation; Long QT syndrome; Patch clamp techniques; Potassium channels; Preclinical methods

Indexed keywords

1 [2 (6 METHYL 2 PYRIDYL)ETHYL] 4 (4 METHYLSULFONYLAMINOBENZOYL)PIPERIDINE; BEPRIDIL; CISAPRIDE; DIPHENHYDRAMINE; ERYTHROMYCIN; FLUOXETINE; HALOPERIDOL; KETANSERIN; LORATADINE; PIMOZIDE; POTASSIUM CHANNEL BLOCKING AGENT; POTASSIUM CHANNEL HERG; QUINIDINE; SOTALOL; TERFENADINE; THIORIDAZINE; VERAPAMIL;

ARTICLE; CELL LINE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG POTENCY; DRUG SAFETY; DRUG SCREENING; HUMAN; HUMAN CELL; IC 50; PATCH CLAMP; RECORDING; ROOM TEMPERATURE; TEMPERATURE SENSITIVITY;

CELLS, CULTURED; DRUG EVALUATION, PRECLINICAL; ELECTRIC STIMULATION; ETHER-A-GO-GO POTASSIUM CHANNELS; HUMANS; INHIBITORY CONCENTRATION 50; PATCH-CLAMP TECHNIQUES; PHARMACEUTICAL PREPARATIONS; POTASSIUM CHANNEL BLOCKERS; POTASSIUM CHANNELS, VOLTAGE-GATED; REPRODUCIBILITY OF RESULTS; TEMPERATURE; TRANSFECTION;

MAMMALIA;

EID: 4644257489     PISSN: 10568719     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.vascn.2004.06.003     Document Type: Article

References (34)

1. A.M. Brown, and D. Rampe Drug-induced long QT syndrome: Is HERG the root of all evil? Pharmaceutical News 7 2000 15 20
2. Ks Therapie 55 2000 195 202
3. + channels in human heart: Comparison with terfenadine under physiological conditions Journal of Pharmacology and Experimental Therapeutics 292 2000 261 264
4. P. Daleau, E. Lessard, M.F. Groleau, and J. Turgeon Erythromycin blocks the rapid component of the delayed rectifier potassium current and lengthens repolarization of guinea pig ventricular myocytes Circulation 91 1995 3010 3016
5. B. Drolet, F. Vincent, J. Rail, M. Chahine, D. Deschenes, S. Nadeau, M. Khalifa, B.A. Hamelin, and J. Turgeon Thioridazine lengthens repolarization of cardiac ventricular myocytes by blocking the delayed rectifier potassium current Journal of Pharmacology and Experimental Therapeutics 288 1999 1261 1268
6. S. Ekins, W.J. Crumb, R.D. Sarazan, J.H. Wikel, and S.A. Wrighton Three-dimensional quantitative structure-activity relationship for inhibition of human ether-a-go-go-related gene potassium channel Journal of Pharmacology and Experimental Therapeutics 301 2002 427 434
7. E. Hanada, H. Ohtani, M. Hirota, N. Uemura, H. Nakaya, H. Kotaki, H. Sato, Y. Yamada, and T. Iga Inhibitory effect of erythromycin on potassium currents in rat ventricular myocytes in comparison with disopyramide Journal of Pharmacy and Pharmacology 55 2003 995 1002
8. ICHS7B Expert Working Group. (February, 2002) Safety pharmacology studies for assessing the potential for delayed ventricular repolarization (QT interval prolongation) by human pharmaceuticals. http://www.ich.org.
9. M. Ishiguro, H. Koga, S. Kohno, T. Hayashi, K. Yamaguchi, and M. Hirota Penetration of macrolides into human polymorphonuclear leucocytes Journal of Antimicrobial Chemotherapy 24 1989 719 729
10. + channel by the neuroleptic pimozide European Journal of Pharmacology 392 2000 137 140
11. M. Khalifa, B. Drolet, P. Daleau, C. Lefez, M. Gilbert, S. Plante, G.E. O'Hara, O. Gleeton, B.A. Hamelin, and J. Turgeon Block of potassium currents in guinea pig ventricular myocytes and lengthening of cardiac repolarization in man by the histamine H1 receptor antagonist diphenhydramine Journal of Pharmacology and Experimental Therapeutics 288 1999 858 865
12. S. Kongsamut, J. Kang, X.L. Chen, J. Roehr, and D. Rampe A comparison of the receptor binding and HERG channel affinities for a series of antipsychotic drugs European Journal of Pharmacology 450 2002 37 41
13. Kr drug response is modulated by KCR1 in transfected cardiac and noncardiac cell lines FASEB Journal 17 2003 2263 2265
14. A.E. Lacerda, J. Kramer, K.Z. Shen, D. Thomas, and A.M. Brown Comparison of block among cloned cardiac potassium channels by non-antiarrhythmic drugs European Heart Journal Supplement 3 2001 K23 K30
15. B. Le Grand, J.M. Talmant, J.P. Rieu, J.F. Patoiseau, F.C. Colpaert, and G.W. John Investigation of the mechanism by which ketanserin prolongs the duration of the cardiac action potential Journal of Cardiovascular Pharmacology 26 1995 803 809
16. + channel by the gastrointestinal prokinetic agent cisapride American Journal of Physiology 273 1997 H2534 H2538
17. H. Numaguchi, F.M. Mullins, J.P. Johnson Jr., D.C. Johns, S.S. Po, I.C. Yang, G.F. Tomaselli, and J.R. Balser Probing the interaction between inactivation gating and dl-sotalol block of hERG Circulation Research 87 2000 1012 1018
18. 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
19. S.S. Po, D.W. Wang, I.C. Yang, J.P. Johnson Jr., L. Nie, and P.B. Bennett Modulation of hERG potassium channels by extracellular magnesium and quinidine Journal of Cardiovascular Pharmacology 33 1999 181 185
20. + channel Journal of Pharmacology and Experimental Therapeutics 299 2001 1007 1012
21. M. Raghoebar, E. Lindeyer, W.B. Van den Berg, and C.A. Van Ginneken On the mechanisms of association of the macrolide antibiotic erythromycin with isolated human polymorphonuclear leucocytes Biochemical Pharmacology 37 1988 3221 3227
22. D. Rampe, M.L. Roy, A. Dennis, and A.M. Brown A mechanism for the proarrhythmic effects of cisapride (Propulsid): High affinity blockade of human cardiac potassium channel hERG FEBS Letters 417 1997 28 32
23. W.S. Redfern, L. Carlsson, A.S. Davis, W.G. Lynch, I. MacKenzie, S. Palethorpe, P.K. Siegl, I. Strang, A.T. Sullivan, R. Wallis, A.J. Camm, and T.G. Hammond 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 Cardiovascular Research 58 2003 32 45
24. + current. Differential sensitivity to block by class III antiarrhythmic agents Journal of General Physiology 96 1990 195 215
25. W.A. Volberg, B.J. Koci, W. Su, J. Lin, and J. Zhou Blockade of human cardiac potassium channel human ether-a-go-go-related gene (HERG) by macrolide antibiotics Journal of Pharmacology and Experimental Therapeutics 302 2002 320 327
26. J. Wang, K. Della Penna, H. Wang, J. Karczewski, T.M. Connolly, K.S. Koblan, P.B. Bennett, and J.J. Salata Functional and pharmacological properties of canine ERG potassium channels American Journal of Physiology 284 2003 H256 H267
27. Ks, in guinea-pig ventricular myocytes British Journal of Pharmacology 128 1999 1733 1738
28. M. Weerapura, S. Nattel, D. Chartier, R. Caballero, and T.E. Hebert A comparison of currents carried by HERG, with and without coexpression of MiRP1, and the native rapid delayed rectifier current. Is MiRP1 the missing link? Journal of Physiology 540 2002 15 27
29. J. Weirich, and H. Antoni Rate-dependence of antiarrhythmic and proarrhythmic properties of class I and class III antiarrhythmic drugs Basic Research in Cardiology 93 Suppl. 1 1998 125 132
30. + channels expressed in mammalian cell lines and Xenopus oocytes Journal of Pharmacological and Toxicological Methods 48 2002 65 80
31. H.J. Witchel, V.K. Pabbathi, G. Hofmann, A.A. Paul, and J.C. Hancox Inhibitory actions of the selective serotonin re-uptake inhibitor citalopram on HERG and ventricular L-type calcium currents FEBS Letters 512 2002 59 66
32. Y.G. Yap, and A.J. Camm Arrhythmogenic mechanisms of non-sedating antihistamines Clinical Experimental and Allergy 29 Suppl. 3 1999 174 181
33. S. Zhang, Z. Zhou, Q. Gong, J.C. Makielski, and C.T. January Mechanism of block and identification of the verapamil binding domain to HERG potassium channels Circulation Research 84 1999 989 998
34. Z. Zhou, Q. Gong, B. Ye, Z. Fan, J.C. Makielski, G.A. Robertson, and C.T. January Properties of hERG channels stably expressed in HEK 293 cells studied at physiological temperature Biophysical Journal 74 1998 230 241