Altering extracellular potassium concentration does not modulate drug block of human ether-a-go-go-related gene (hERG) channels

Clinical and Experimental Pharmacology and Physiology

Volumn 33, Issue 11, 2006, Pages 1059-1065

  Limberis, James T ^a   Su, Zhi ^a   Cox, Bryan F ^a   Gintant, Gary A ^a   Martin, Ruth L ^a  

^a ABBOTT LABORATORIES   (United States)

Author keywords

Cardiac repolarization; Human ether a go go related gene (hERG); Hypokalaemia; Repolarization reserve; Torsades de Pointes

Indexed keywords

DOFETILIDE; MESORIDAZINE; POTASSIUM; POTASSIUM CHANNEL BLOCKING AGENT; POTASSIUM CHANNEL HERG; QUINIDINE; TERFENADINE;

ARTICLE; CELL STRAIN HEK293; CONTROLLED STUDY; DISEASE ASSOCIATION; EMBRYO; HEART REPOLARIZATION; HUMAN; HUMAN CELL; HYPOKALEMIA; IC 50; LONG QT SYNDROME; POTASSIUM CELL LEVEL; POTASSIUM CURRENT; RISK FACTOR; TORSADE DES POINTES; VOLTAGE CLAMP;

CELL LINE; ETHER-A-GO-GO POTASSIUM CHANNELS; HUMANS; KIDNEY; MESORIDAZINE; PHENETHYLAMINES; POTASSIUM; POTASSIUM CHANNEL BLOCKERS; QUINIDINE; SULFONAMIDES; TERFENADINE;

EID: 33750092224     PISSN: 03051870     EISSN: 14401681     Source Type: Journal    
DOI: 10.1111/j.1440-1681.2006.04487.x     Document Type: Article

References (22)

1. Goldfarb S, Ziyadeh FN. Renal diseases, fluid and electrolyte disorders, and hypertension. In: Myers AR (ed.). Medicine, 4th edn. Lippincott Williams & Wilkins, Philadelphia. 2000; 360-2.
2. Zeltser D, Justo D, Halkin A, Prokhorov V, Heller K, Viskin S. Torsade de Pointes due to noncardiovascular drugs: Most patients have easily identifiable risk factors. Medicine 2003; 82: 282-90.
3. Kr blockers dofetilide, D-sotalol, E-4031, and MK-499. J. Cardiovasc. Pharmacol. 1998; 24: 199-208.
4. Yang T, Tande P, Lathrop D, Refsum H. Effects of altered extracellular potassium and pacing cycle length on the class III antiarrhythmic actions of dofetilide (UK-68,798) in guinea-pig papillary muscle. Cardiovasc. Drugs Ther. 1992; 6: 429-36.
5. Marschang H, Beyer T, Karolyi L, Kubler W, Brachmann J. Differential rate and potassium-dependent effects of the class III agents D-sotalol and dofetilide on guinea pig papillary muscle. Cardiovasc. Drugs Ther. 1998; 12: 573-83.
6. Kr: Implications for Torsade de Pointes and reverse use dependence. Circulation 1996; 93: 407-11.
7. Yang B, Xu D, Xu C et al. Inactivation gating determines drug potency: A common mechanism for drug blockade of HERG channels. Acta Pharmacol. Sin. 2004; 25: 554-60.
8. Mergenthaler J, Haverkamp W, Huttenhofer A et al. Blocking effects of the antiarrhythmic drug propafenone on the HERG potassium channel. Naunyn Schmiedebergs Arch. Pharmacol. 2001; 363: 472-80.
9. 3H] dofetilide binding to cardiac myocytes: Modulation by extracellular potassium. J. Mol. Cell. Cardiol. 1997; 29: 183-91.
10. o. J. Pharmacol. Toxicol. Methods 2004; 50: 187-99.
11. Zhou Z, Gong Q, Ye B et al. Properties of hERG channels stably expressed in HEK 293 cells studied at physiological temperature. Biophys. J. 1998; 74: 230-41.
12. Tao H, Santa Ana D, Guia A et al. Automated tight seal electrophysiology for assessing the potential hERG liability of pharmaceutical compounds. Assay Drug Dev. Technol. 2004; 2: 497-506.
13. Guo L, Guthrie H. Automated electrophysiology in the preclinical evaluation of drugs for potential QT prolongation. J. Pharmacol. Toxicol. Methods 2005; 52: 123-35.
14. Dubin A, Nasser N, Rohrbacher J et al. Identifying modulators of hERG channel activity using the PatchXpress planar patch clamp. J. Biomol. Screen. 2005; 10: 168-81.
15. Hille B. Introduction: Ohms law is central. In: Hille B (ed.). Ionic Channels of Excitable Membranes, 2nd edn. Sinauer Associates, Sunderland. 1992; 1-19.
16. Foster J, Bhambra P, Darwich O, Miller A. Block of hERG by cisapride and quinidine in different extracellular electrolyte solutions. Biophys. J. 2005; 88: A609 (Abstract).
17. Kr channels minimally comprise hERG 1a and 1b subunits. J. Biol. Chem. 2004; 279: 44 690-4.
18. Kr. Nature 1997; 388: 289-92.
19. Abbott G, Sesti F, Splawski I et al. MiRP1 forms Ikr potassium channels with HERG and is associated with cardiac arrhythmia. Cell 1999; 97: 175-87.
20. Weerapura M, Nattel S, Chartier D, Caballero R, Hebert TE. 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? J. Physiol. 2002; 540: 15-27.
21. + current in isolated canine cardiac Purkinje myocytes. Biophys. J. 1987; 52: 519-25.
22. Roden D. Taking the 'idio' out of 'idiosyncratic': Predicting Torsade de Pointes. Pacing Clin. Electrophysiol. 1998; 21: 1029-34.