K201, a multi-channel blocker, inhibits clofilium-induced torsades de pointes and attenuates an increase in repolarization

European Journal of Pharmacology

Volumn 555, Issue 1, 2007, Pages 54-60

  Hasumi, Hisashi ^a   Matsuda, Ryuko ^a   Shimamoto, Ken ^b   Hata, Yoshihito ^a   Kaneko, Noboru ^a  

^a DOKKYO MEDICAL UNIVERSITY   (Japan)

^b TOKYO WOMEN'S MEDICAL UNIVERSITY   (Japan)

Author keywords

1 Adrenoceptor blocker; Clofilium; K201 (JTV 519); Multi channel blocker; QT interval prolongation; Torsades de pointes

Indexed keywords

4 [3 (4 BENZYL 1 PIPERIDINYL)PROPIONYL] 2,3,4,5 TETRAHYDRO 7 METHOXY 1,4 BENZOTHIAZEPINE; CLOFILIUM; METHOXAMINE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTINUOUS INFUSION; CONTROLLED STUDY; DOSE RESPONSE; DRUG EFFECT; HEART REPOLARIZATION; MALE; NONHUMAN; PRIORITY JOURNAL; QT INTERVAL; QT PROLONGATION; TORSADE DES POINTES;

ADRENERGIC ALPHA-AGONISTS; ANIMALS; ANTI-ARRHYTHMIA AGENTS; BLOOD PRESSURE; CALCIUM CHANNEL BLOCKERS; CARDIOTONIC AGENTS; ELECTROCARDIOGRAPHY; HEART RATE; LONG QT SYNDROME; MALE; METHOXAMINE; POTASSIUM CHANNEL BLOCKERS; QUATERNARY AMMONIUM COMPOUNDS; RABBITS; RECEPTORS, ADRENERGIC, ALPHA-1; SODIUM CHANNEL BLOCKERS; THIAZEPINES; TORSADES DE POINTES;

EID: 33845807838     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2006.10.005     Document Type: Article

References (35)

1. Antzelevitch C. Arrhythmogenic mechanisms of QT prolonging drugs: is QT prolongation really the problem?. J. Electrocardiol. 37 (2004) 15-24 (Suppl)
2. Antzelevitch C., Belardinelli L., Zygmunt A.C., Burashnikov A., Di Diego J.M., Fish J.M., Cordeiro J.M., and Thomas G. Electrophysiological effects of ranolazine, a novel antianginal agent with antiarrhythmic properties. Circulation 110 (2004) 904-910
3. Bazett H.C. An analysis of the time-relations of electrocardiograms. Heart 7 (1920) 353-370
4. Bednar M.M., Harrigan E.P., Anziano R.J., Camm A.J., and Ruskin J.N. The QT interval. Prog. Cardiovasc. Dis. 43 Suppl 1 (2001) 1-45
5. Berridge M.J. Inositol triphosphate and deacylglycerol as second messenger. Biochem. J. 220 (1984) 345-360
6. Carlsson L., Almgren O., and Duker G. QTU-prolongation and torsades de pointes induced by putative class III antiarrhythmic agents in the rabbit: etiology and interventions. J. Cardiovasc. Pharmacol. 16 (1990) 276-285
7. Carlsson L., Amos G.J., Andersson B., Drews L., Duker G., and Wadstedt G. Electrophysiological characterization of the prokinetic agents cispride and mosapride in vivo and in vitro: implications for proarrhyyjmic potential?. J. Pharmacol. Exp. Ther. 282 (1997) 220-227
8. De Ponti F., Poluzzi E., Cavalli A., Recanatini M., and Montanaro N. Safety of non-antiarrhythmic drugs that prolong the QT interval or induce torsade de poites. An overview. Drug Safety 25 (2002) 263-286
9. Farr M.A., and Basson C.T. Sparking the failing heart. N. Engl. J. Med. 351 (2004) 185-187
10. Haddad P.M., and Anderson I.M. Antipsychotic-related QTc prolongation, torsade de pointes and sudden death. Drugs 62 (2002) 1649-1671
11. Hollingshead L.M., Faulds D., and Fitton A. Bepridil. A review of its pharmacological properties and therapeutic use in stable angina pectoris. Drugs 44 (1992) 835-857
12. Inagaki K., Kihara Y., Hayashida W., Izumi T., Iwanaga Y., Yoneda T., Takeuchi Y., Suyama K., Muso E., and Sasayama S. Anti-ischemic effect of a novel cardioprotective agent, JTV519, is mediated through specific activation of δ-isoform of protein kinase C in rat ventricular myocardium. Circulation 101 (2000) 797-804
13. Ito K., Shigematsu S., Sato T., Abe T., Li Y., and Arita M. JTV-519, a novel cardioprotective agent, improves the contractile recovery after ischaemia-reperfusion in coronary perfused guinea-pig ventricular muscles. Br. J. Pharmacol. 130 (2000) 767-776
14. Kaneko N. New 1,4-benzothiazepine derivative, K201, demonstrates cardioprotective effects against sudden cardiac cell death and intracellular calcium blocking action. Drug Dev. Res. 33 (1994) 429-438
15. Kaneko N., Ago H., Matsuda R., Inagaki E., and Miyama M. Crystal structure of annexin V with its ligand K-201 as a calcium channel activity inhibitor. J. Mol. Biol. 274 (1997) 16-20
16. Kawabata H., Ryomoto T., and Ishikawa K. Effect of a novel cardioprotective agent, JTV-519, on metabolism, contraction and relaxation in the ischemia-reperfused rabbit heart. Jpn. Circ. J. 64 (2000) 772-776
17. Kimura J., Kawahara M., Sakai E., Yatabe J., and Nakanishi H. Effects of a novel cardioprotective drug, JTV-519, on membrane currents of guinea pig ventricular myocytes. Jpn. J. Pharmacol. 79 (1999) 275-281
18. + current in guinea-pig ventricular myocytes. Naunyn-Schmiedeberg's Arch. Pharmacol. 361 (2000) 646-653
19. Kumagai K., Nakashima H., Gondo N., and Saku K. Antiarrhythmic effects of JTV-519, a novel cardioprotective drug, on atrial fibrillation/flutter in a canine sterile pericarditis model. J. Cardiovasc. Electrophysiol. 14 (2003) 880-884
20. 1-adrenoceptor stimulation. J. Cardiovasc. Pharmacol. 36 (2000) 728-736
21. Matsuda T., Matsuda R., Taguchi I., Toyoda S., and Kikuchi M. A novel cardioprotective drug, K201 (JTV519), induced prolongation of QT and QTc intervals, but not torsades de pointes. Dokkyo J. Med. Sci. 33 (2006) 17-24
22. Mazur A., Roden D.M., and Anderson M.E. Systemic administration of calmodulin antagonist W-7 or protein kinase A inhibitor H-8 prevents torsade de pointes in rabbits. Circulation 100 (1999) 2437-2442
23. Mirvis D.M., and Goldberger A.L. Electrocardiography. In: Zipes D.S., Libby P., Bonow R.O., and Braumwald E. (Eds). Braumwald's Heart Disease. A Textbook of Cardiovascular Medicine. 7th ed. (2005), Elsevier, Philadelpia 118
24. Nakaya H., Furusawa Y., Ogura T., Tamagawa M., and Uemura H. Inhibitory effects of JTV-519, a novel cardioprotective drug, on potassium currents and experimental atrial fibrillation in guinea-pig hearts. Br. J. Pharmacol. 131 (2000) 1363-1372
25. Nobe S., Aomine M., and Arita M. Bepridil prolongs the action potential duration of guinea pig ventricular muscle only at rapid rates of stimulation. Gen. Pharmacol. 24 (1993) 1187-1196
26. Olgin J.E., and Zipes D.P. Specific arrhythmias: diagnosis and treatment. In: Zipes D.S., Libby P., Bonow R.O., and Braumwald E. (Eds). Braumwald's Heart Disease. A Textbook of Cardiovascular Medicine. 7th ed. (2005), Elsevier, Philadelpia 838
27. Roden D.M. Drug-induced prolongation of the QT interval. N. Engl. J. Med. 350 (2004) 1013-1022
28. Singh B.N. Antiarrhythmic actions of amiodarone: a profile of a paradoxical agent. Am. J. Cardiol. 78 Suppl 4A (1996) 41-53
29. Straus S.M., Kors J.A., De Bruin M.L., van der Hooft C.S., Hofman A., Heeringa J., Deckers J.W., Kingma J.H., Sturkenboom M.C., Stricker B.H., and Witteman J.C. Prolonged QTc interval and risk of sudden cardiac death in a population of older adults. J. Am. Coll. Cardiol. 47 (2006) 362-367
30. Thibault B., and Nattel S. Optimal management with class I and class III antiarrhythmic drugs should be done in the outpatient setting: protagonist. J. Cardiovasc. Electrophysiol. 10 (1999) 472-481
31. Wehrens X.H., and Marks A.R. Novel therapeutic approaches for heart failure by normalizing calcium cycling. Nat. Rev. Drug Discov. 3 (2004) 565-573
32. Wehrens X.H., Lehnart S.E., Reiken S.R., Deng S.-X., Vest J.A., Cervantes D., Coromilas J., Landry D.W., and Marks A.R. Protection from cardiac arrhythmia through ryanodine receptor-stabilizing protein calstanbin2. Science 304 (2004) 292-296
33. Wu L., Shryock J.C., Song Y., Li Y., Antzelevitch C., and Belardinelli L. Antiarrhythmic effects of ranolazine in a guinea pig in vitro model of long-QT syndrome. J. Pharmacol. Exp. Ther. 310 (2004) 599-605
34. Wu L., Shryock J.C., Song Y., and Belardinelli L. An increase in late sodium current potentiates the proarrhythmic activities of low-risk QT-prolongating drugs in female rabbit hearts. J. Pharmacol. Exp. Ther. 316 (2006) 718-726
35. Zipes D.P., and Wellens H.J.J. Sudden cardiac death. Circulation 98 (1998) 2334-2351