State dependent dissociation of HERG channel inhibitors

British Journal of Pharmacology

Volumn 151, Issue 8, 2007, Pages 1368-1376

  Stork, D ^a   Timin, E N ^a   Berjukow, S ^a   Huber, C ^a   Hohaus, A ^a   Auer, M ^b   Hering, S ^a  

^a UNIVERSITY OF VIENNA   (Austria)

^b Novartis Inst Biomed Res Vienna   (Austria)

Author keywords

Drug trapping; HERG; HERG channel blocker; Use dependent block

Indexed keywords

1 [2 (6 METHYL 2 PYRIDYL)ETHYL] 4 (4 METHYLSULFONYLAMINOBENZOYL)PIPERIDINE; AMIODARONE; BEPRIDIL; BLOCKING AGENT; CISAPRIDE; DOMPERIDONE; DROPERIDOL; HALOPERIDOL; POTASSIUM CHANNEL HERG; POTASSIUM CHANNEL HERG INHIBITOR; TERFENADINE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; DISSOCIATION; ELECTRIC POTENTIAL; ELECTRODE; FEMALE; HETEROLOGOUS EXPRESSION; NONHUMAN; OOCYTE; PRIORITY JOURNAL; PROTEIN EXPRESSION; VOLTAGE CLAMP; XENOPUS;

ACTION POTENTIALS; ANIMALS; ARRHYTHMIA; DOSE-RESPONSE RELATIONSHIP, DRUG; ELECTRIC STIMULATION; ETHER-A-GO-GO POTASSIUM CHANNELS; HEART VENTRICLES; HUMANS; INHIBITORY CONCENTRATION 50; KINETICS; MUTATION; OOCYTES; PATCH-CLAMP TECHNIQUES; XENOPUS;

EID: 34547902408     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1038/sj.bjp.0707356     Document Type: Article

References (32)

1. Armstrong CM (1971). Interaction of tetraethylammonium ion derivatives with the potassium channels of giant axon. J Gen Physiol 58: 413-437.
2. Baburin I, Beyl S, Hering S (2006). Automated fast perfusion of Xenopus oocytes for drug screening. Pflügers Arch 453: 117-123.
3. + current in cardiac myocytes by dofetilide. J Pharmacol Exp Ther 262: 809-817.
4. Kr of guinea pig cardiomyocytes by antipsychotic drug trifluoperazine. J Pharmacol Exp Ther 313: 888-895.
5. Curran ME, Splawski I, Timothy KW, Vincent GM, Green ED, Keating MT (1995). A molecular basis for cardiac arrhythmia: HERG mutations cause long QT syndrome. Cell 80: 795-803.
6. De Bruin ML, Pettersson M, Meyboom RH, Hoes AW, Leufkens HG (2005). Anti-HERG activity and the risk of drug-induced arrhythmias and sudden death. Eur Heart J 26: 590-597.
7. Fermini B, Fossa AA (2003). The impact of drug-induced QT interval prolongation on drug discovery and development. Nat Rev Drug Discov 2: 439-447.
8. Grabner M, Wang Z, Hering S, Striessnig J, Glossmann H (1996). Transfer of 1,4-dihydropyridine sensitivity from L-type to class A (BI) calcium channels. Neuron 16: 207-218.
9. Ishii K, Nagai M, Takahashi M, Endoh M (2003). Dissociation of E-4031 from the HERG channel caused by mutations of an amino acid results in greater block at high stimulation frequency. Cardiovasc Res 57: 651-659.
10. + channel by the antidepressant drug amitriptyline. Br J Pharmacol 129: 1474-1480.
11. Kamiya K, Niwa R, Mitcheson JS, Sanguinetti MC (2006). Molecular determinants of HERG channel block. Mol Pharmacol 69: 1709-1716.
12. Keating MT, Sanguinetti MC (2001). Molecular and cellular mechanisms of cardiac arrhythmias. Cell 104: 569-580.
13. Kiehn J, Thomas D, Karle CA, Schols W, Kubler W (1999). Inhibitory effects of the class III antiarrhythmic drug amiodarone on cloned HERG potassium channels. Naunyn Schmiedebergs Arch Pharmacol 359: 212-219.
14. + current by antifungal drug miconazole. Br J Pharmacol 144: 840-848.
15. Kirsch GE, Trepakova ES, Brimecombe JC, Sidach SS, Erickson HD, Kochan MC et al. (2004). Variability in the measurement of HERG potassium channel inhibition: effects of temperature and stimulus pattern. J Pharmacol Toxicol Methods 50: 93-101.
16. Kushida S, Ogura T, Komuro I, Nakaya H (2002). Inhibitory effect of the class III antiarrhythmic drug nifekalant on HERG channels: mode of action. Eur J Pharmacol 457: 19-27.
17. Mitcheson JS, Chen J, Lin M, Culberson C, Sanguinetti MC (2000). A structural basis for drug-induced long QT syndrome. Proc Natl Acad Sci USA 97: 12329-12333.
18. + channel. A model for bad behavior. J Med Chem 46: 2017-2022.
19. + channel blockade: current knowledge and strategies for the early prediction during drug development. Med Res Rev 25: 133-166.
20. Redfern WS, Carlsson L, Davis AS, Lynch WG, Mackenzie I, Palethorpe S et al. (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.
21. Kr potassium channel. Cell 81: 299-307.
22. Sanguinetti MC, Mitcheson JS (2005). Predicting drug-HERG channel interactions that cause acquired long QT syndrome. Trends Pharmacol Sci 26: 119-124.
23. Suessbrich H, Waldegger S, Lang F, Busch AE (1996). Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole. FEBS Lett 385: 77-80.
24. Suessbrich H, Schönherr R, Heinemann SH, Attali B, Lang F, Busch AE (1997). The inhibitory effect of the antipsychotic drug haloperidol on HERG potassium channels expressed in Xenopus oocytes. Br J Pharmacol 120: 968-974.
25. Trudeau MC, Warmke JW, Ganetzky B, Robertson GA (1995). HERG, a human inward rectifier in the voltage-gated potassium channel family. Science 269: 92-95.
26. Kr: the HERG channel. J Mol Cell Cardiol 33: 835-849.
27. Tsujimae K, Suzuki S, Yamada M, Kurachi Y (2004). Comparison of kinetic properties of quinidine and dofetilide block of HERG channels. Eur J Pharmacol 493: 29-40.
28. + channels: friend and foe. Trends Pharmacol Sci 22: 240-246.
29. + channels expressed in Xenopus oocytes. Cell Physiol Biochem 9: 81-89.
30. Walker BD, Singleton CB, Bursill JA, Wyse KR, Valenzuela SM, Qiu MR et al. (1999). Inhibition of the human ether-a-go-go-related gene (HERG) potassium channel by cisapride: affinity for open and inactivated states. Br J Pharmacol 128: 444-450.
31. Witchel HJ, Dempsey CE, Sessions RB, Perry M, Milnes JT, Hancox JC et al. (2004). The low-potency, voltage-dependent HERG blocker propafenone-molecular determinants and drug trapping. Mol Pharmacol 66: 1201-1212.
32. Zhang S, Zhou Z, Gong Q, Makielski JC, January CT (1999). Mechanism of block and identification of the verapamil binding domain to HERG potassium channels. Circ Res 84: 989-998.