Effects of an hERG activator, ICA-105574, on electrophysiological properties of canine hearts

Journal of Pharmacological Sciences

Volumn 121, Issue 1, 2013, Pages 1-8

  Asayama, Mahoko ^a,b   Kurokawa, Junko ^a   Shirakawa, Kiyoshi ^b   Okuyama, Hisashi ^b   Kagawa, Toshiki ^b   Okada, Jun Ichi ^c   Sugiura, Seiryo ^c   Hisada, Toshiaki ^c   Furukawa, Tetsushi ^a  

^a TOKYO MEDICAL AND DENTAL UNIVERSITY   (Japan)

^b MITSUBISHI TANABE PHARMA CORPORATION   (Japan)

^c UNIVERSITY OF TOKYO   (Japan)

Author keywords

HERG activator; IKr channel; KCNH2; Pro arrhythmia; QT and QTc interval

Indexed keywords

ICA 105574; POTASSIUM CHANNEL HERG; POTASSIUM CHANNEL STIMULATING AGENT; UNCLASSIFIED DRUG;

ACTION POTENTIAL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG DOSE COMPARISON; DRUG EFFECT; DRUG MEGADOSE; DRUG PROTEIN BINDING; ELECTROCARDIOGRAPHY MONITORING; EMBRYO; EXPERIMENTAL DOG; EXPERIMENTAL GUINEA PIG; EXPERIMENTAL MODEL; GENE ACTIVATION; HEART DEPOLARIZATION; HEART ELECTROPHYSIOLOGY; HEART RATE; HUMAN; HUMAN CELL; IN VIVO STUDY; ISOLATED HEART; MALE; NONHUMAN; PATCH CLAMP; PULSE RATE; QRS COMPLEX; QT INTERVAL; SHORT QT INTERVAL; STABLE EXPRESSION; TIME TO MAXIMUM PLASMA CONCENTRATION;

EID: 84873876920     PISSN: 13478613     EISSN: 13478648     Source Type: Journal    
DOI: 10.1254/jphs.12220FP     Document Type: Article

References (30)

1. Sanguinetti MC, Jiang C, Curran ME, Keating MT. A mechanistic link between an inherited and an acquired cardiac arrhythmia: HERG encodes the IKr potassium channel. Cell. 1995;81: 299-307.
2. Clancy CE, Rudy Y. Cellular consequences of HERG mutations in the long QT syndrome: precursors to sudden cardiac death. Cardiovasc Res. 2001;50:301-313.
3. Clancy CE, Kurokawa J, Tateyama M, Wehrens XH, Kass RS. K+ channel structure-activity relationships and mechanisms of drug-induced QT prolongation. Annu Rev Pharmacol Toxicol. 2003;43:441-461.
4. Brugada R, Hong K, Dumaine R, Cordeiro J, Gaita F, Borggrefe M, et al. Sudden death associated with short-QT syndrome linked to mutations in HERG. Circulation. 2004;109:30-35.
5. Gerlach AC, Stoehr SJ, Castle NA. Pharmacological removal of human ether-a-go-go-related gene potassium channel inactivation by 3-nitro-N-(4-phenoxyphenyl) benzamide (ICA-105574). Mol Pharmacol. 2010;77:58-68.
6. Garg V, Stary-Weinzinger A, Sachse F, Sanguinetti MC. Molecular determinants for activation of human ether-a-go-go-related gene 1 potassium channels by 3-nitro-n-(4-phenoxyphenyl) benzamide. Mol Pharmacol. 2011;80:630-637.
7. Kurokawa J, Tamagawa M, Harada N, Honda S, Bai CX, Nakaya H, et al. Acute effects of oestrogen on the guinea pig and human IKr channels and drug-induced prolongation of cardiac repolarization. J Physiol. 2008;586:2961-2973.
8. Hamlin RL, Cruze CA, Mittelstadt SW, Kijtawornrat A, Keene BW, Roche BM, et al. Sensitivity and specificity of isolated perfused guinea pig heart to test for drug-induced lengthening of QTc. J Pharmacol Toxicol Methods. 2004;49:15-23.
9. Van de Water A, Verheyen J, Xhonneux R, Reneman RS. An improved method to correct the QT interval of the electrocardiogram for changes in heart rate. J Pharmacol Methods. 1989;22: 207-217.
10. Bazzet H. An analysis of the time relationship of electrocardiograms. Heart. 1920;7:353.
11. Fridericia LS. Die Systolendauer im elektrokardiogramm bei normalen menschen und bei herzkranken. Acta Med Scand. 1920;53:489.
12. Sugiyama A, Hashimoto K. Effects of gastrointestinal prokinetic agents, TKS159 and cisapride, on the in situ canine heart assessed by cardiohemodynamic and electrophysiological monitoring. Toxicol Appl Pharmacol. 1998;152:261-269.
13. Nakai D, Kumamoto K, Sakikawa C, Kosaka T, Tokui T. Evaluation of the protein binding ratio of drugs by a micro-scale ultracentrifugation method. J Pharm Sci. 2004;93:847-854.
14. Schonherr R, Heinemann SH. Molecular determinants for activation and inactivation of HERG, a human inward rectifier potassium channel. J Physiol. 1996;493:635-642.
15. Smith PL, Baukrowitz T, Yellen G. The inward rectification mechanism of the HERG cardiac potassium channel. Nature. 1996;379:833-836.
16. Redfern WS, Carlsson L, Davis AS, Lynch WG, MacKenzie I, Palethorpe S, et al. 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. 2003; 58:32-45.
17. Perry M, Sanguinetti M, Mitcheson J. Revealing the structural basis of action of hERG potassium channel activators and blockers. J Physiol. 2010;588:3157-3167.
18. Kang J, Chen XL, Wang H, Ji J, Cheng H, Incardona J, et al. Discovery of a small molecule activator of the human ether-ago-go-related gene (HERG) cardiac K+ channel. Mol Pharmacol. 2005;67:827-836.
19. Perry M, Sachse FB, Sanguinetti MC. Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator. Proc Natl Acad Sci U S A. 2007;104:13827-13832.
20. Zhou J, Augelli-Szafran CE, Bradley JA, Chen X, Koci BJ, Volberg WA, et al. Novel potent human ether-a-go-go-related gene (hERG) potassium channel enhancers and their in vitro antiarrhythmic activity. Mol Pharmacol. 2005;68:876-884.
21. Xu X, Recanatini M, Roberti M, Tseng GN. Probing the binding sites and mechanisms of action of two human ether-a-go-go-related gene channel activators, 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643) and 2-[2-(3,4-dichloro-phenyl)-2,3-dihydro-1H-isoindol-5-ylamino]-nicotinic acid (PD307243). Mol Pharmacol. 2008;73:1709-1721.
22. Casis O, Olesen SP, Sanguinetti MC. Mechanism of action of a novel human ether-a-go-go-related gene channel activator. Mol Pharmacol. 2006;69:658-665.
23. Hansen RS, Diness TG, Christ T, Demnitz J, Ravens U, Olesen SP, et al. Activation of human ether-a-go-go-related gene potassium channels by the diphenylurea 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643). Mol Pharmacol. 2006;69: 266-277.
24. Su Z, Limberis J, Souers A, Kym P, Mikhail A, Houseman K, et al. Electrophysiologic characterization of a novel hERG channel activator. Biochem Pharmacol. 2009;77:1383-1390.
25. Roden DM. Principles in pharmacogenetics. Epilepsia. 2001; 42 Suppl 5:44-48.
26. Shibata S, Okamoto Y, Endo S, Ono K. Direct effects of esmolol and landiolol on cardiac fuction, coronary vasoactivity, and ventricular electrophysiology in guinea-pig hearts. J Pharmacol Sci. 2012;118:255-265.
27. Nishida A, Takizawa T, Matsumoto A, Miki T, Seino S, Nakaya H. Inhibition of ATP-sensitive K+ channels and L-type Ca2+ channels by amiodarone elicits contradictory effect in insulin secretion in MIN6 cells. J Pharmacol Sci. 2011;116:73-80.
28. Takahara A, Sugiyama A, Hashimoto K. Reduction of repolarization reserve by halothane anaesthesia sensitizes the guinea-pig heart for drug-induced QT interval prolongation. Br J Pharmacol. 2005;146:561-567.
29. Bjerregaard P, Nallapaneni H, Gussak I. Short QT interval in clinical practice. J Electrocardiol. 2010;43:390-395.
30. Viskin S, Zeltser D, Ish-Shalom M, Katz A, Glikson M, Justo D, et al. Is idiopathic ventricular fibrillation a short QT syndrome? Comparison of QT intervals of patients with idiopathic ventricular fibrillation and healthy controls. Heart Rhythm. 2004;1: 587-591.