Blockers of the Kv1.5 channel for the treatment of atrial arrhythmias

Expert Opinion on Therapeutic Patents

Volumn 12, Issue 11, 2002, Pages 1589-1598

  Brendel, Joachim ^a   Peukert, Stefan ^a  

^a SANOFI AVENTIS DEUTSCHLAND GMBH   (Germany)

Author keywords

Arrhythmia; Atrial fibrillation; IKur; Kv1.5; Potassium channel blockers

Indexed keywords

AMBASILIDE; AMIDE; ANTIARRHYTHMIC AGENT; AZIMILIDE; BEPRIDIL; BIPHENYL DERIVATIVE; BISINDOLYLMALEIMIDE; BUPIVACAINE; CARBAMIC ACID DERIVATIVE; CHROMAN DERIVATIVE; CLOTRIMAZOLE; CROMAKALIM; DOFETILIDE; ERYTHROMYCIN; EXTINA; IBUTILIDE FUMARATE; INDAN DERIVATIVE; KETOCONAZOLE; LEMAKALIM; LORATADINE; N [3 HYDROXY 2,2 DIMETHYL 6 (4,4,4 TRIFLUOROBUTOXY)CHROMAN 4 YL] N METHYLMETHANESULFONAMIDE; NIFEDIPINE; NIP 142; POTASSIUM CHANNEL BLOCKING AGENT; PYRIDAZINONE DERIVATIVE; QUINIDINE GLUCONATE; QUINOLINE DERIVATIVE; S 20951; S 9947; SOTALOL; THIAZOLIDINE DERIVATIVE; TYKOSYN; UNCLASSIFIED DRUG; UNINDEXED DRUG; VERAPAMIL; VOLTAGE GATED POTASSIUM CHANNEL; ZATEBRADINE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIARRHYTHMIC ACTIVITY; CARDIOLOGY; CHEMISTRY; CHO CELL; CLINICAL PRACTICE; DOG; DRUG EFFECT; DRUG EFFICACY; DRUG SAFETY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG TARGETING; HEART ATRIUM ARRHYTHMIA; HUMAN; HUMAN CELL; IN VIVO STUDY; NONHUMAN; PATENT; RAT; REVIEW; SIDE EFFECT;

EID: 0036848462     PISSN: 13543776     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543776.12.11.1589     Document Type: Review

References (49)

1. KANNEL WB, WOLF PA, BENJAMIN EJ, LEVY D: Prevalence, incidence, prognosis and predisposing conditions for atrial fibrillation: population based estimates. Am. J. Cardiol (1998) 82:2N-9N.
2. GERLACH U: IKs channel blockers: potential antiarrhythmic agents. Drugs Fut. (2001) 26:473-484.
3. PRATT CM, MOYE LA: The cardiac arrhythmia suppression trial: background, interim results and implications. Am. J. Cardiol. (1990) 65(4):20B-29B.
4. WALDO AL, CAMM AJ, DERUYTER H et al.: Effect of d-sotalol on mortality in patients with left ventricular dysfunction after recent and remote myocardial infarction. Lancet (1996) 348:7-12.
5. BRIL A: Recent advances in arrhythmia therapy: treatment and prevention of atrial fibrillation. Curr. Opin. Pharmacol. (2002) 2(2):154-159.
6. NATTEL S, HADJIS T, TALAJIC M: The treatment of atrial fibrillation. Drugs (1994) 48:345-371.
7. + currents in isolated guinea-pig cardiomyocytes. Jpn. J. Pharmacol. (2000) 82:1-12.
8. + current in human ventricular myocytes. Circ. Res. (1996) 78:689-696.
9. + current in cultured adult human atrial myocytes. Circ. Res. (1997) 80:572-579.
10. AMOS GJ, WETTWER E, METZGER F, Ll Q, HIMMEL HM, RAVENS U: Differences between outward currents of human atrial and subepicardial ventricular myocytes. J. Physiol. (Lond.) (1996) 491:31-50.
11. + channel current. Circ. Res. (1993) 73:210-216.
12. WANG Z, FERMINI B, NATTEL S: Sustained depolarisation-induced outward current in human atrial myocytes. Circ. Res. (1993) 73:1061-1076.
13. NATTEL S, YUE L, WANG Z: Cardiac ultrarapid delayed rectifiers. Cell Physiol. Biochem. (1999) 9:217-226.
14. ASHCROFT MA: Voltage gated K+ channels. In: Ion channels and disease. Academic Press, London (2000):97-123.
15. FENG J, XU D, WANG Z, NATTEL S: Ultrarapid delayed rectifier current inactivation in human atrial myocytes: properties and consequences. Am. J. Physiol. (1998) 275:H1717-H1725.
16. SCHAFFER P, PELZMANN B, BERNHART E, LANG P, LÖKEBÖ JE, MÄCHLER H et al.: Estimation of outward currents in isolated human atrial myocytes using inactivation time course analysis. Pflügers Arch. Eur. J. Physiol. (1998) 436:457-468.
17. NYGREN A, LEON LJ, GILES WR: Simulations of the human atrial action potential. Phil. Trans. R. Soc. Lond. A. (2001) 359:1111-1125.
18. NYGREN A, FISET C, FIREK L, CLARK JW, LINDBLAD DS, CLARK RB et al.: Mathematical model of an adult human atrial cell. Circ. Res. (1998) 82:63-81.
19. COURTEMANCHE M, RAMIREZ RJ, NATTEL S: Ionic targets for drug therapy and atrial fibrillation-induced electrical remodelling: insights from a mathematical model. Cardiovasc. Res. (1999) 42:477-489.
20. WANG Z, FERMINI B, NATTEL S: Effects of flecainide, quinidine, and 4-aminopyridine on transient outward and ultrarapid delayed rectifier currents in human atrial myocytes. J Pharmacol. Exp. Ther. (1995) 272:184-196.
21. FRANQUEZA L, VALENZUELA C, DELPON E, LONGOBARDO M, CABALLERO R, TAMARGO J: Effects of propafenone and 5-hydroxy-propafenone on hKv1.5 channels. Br. J. Pharmacol. (1998) 125:969-978.
22. GROSS GJ, CASTLE NA: Propafenone inhibition of human atrial myocyte repolarizing currents. J. Mol. Cell. Cardiol. (1998) 30:783-793.
23. SEKI A, HAGIWARI N, KASANUKI H: Effects of propafenone on K currents in human atrial myocytes. Br. J. Pharmacol. (1999) 126:1153-1162.
24. KOBAYASHI S, REIEN Y, OGURA T, SAITO T, MASUDA Y, NAKAYA H: Inhibitory effect of bepridil on hKv1.5 channel current: comparison with amiodarone and E-4031. Eur. J. Pharmacol. (2001) 430:149-157.
25. STEID JV, YOOL AJ: Distinct mechanisms of block of Kv1.5 channels by tertiary and quaternary amine clofilium compounds. Biophysical Journal (2001) 81(5):2606-2613.
26. IFTINCA M, WALDRON GJ, TRIGGLE CR, COLE WC: State-dependent block of rabbit vascular smooth muscle delayed rectifier and Kv1.5 channels by inhibitors of cytochrome P450-dependent enzymes. J. Pharmacol. Exp. Ther. (2001) 296:718-728.
27. + channels. J. Pharmacol. Exp. Ther. (2001) 296:573-583.
28. + channel Kv1.5 by the antibiotic erythromycin. Nau. Schmied. Arch. Pharmacol. (1997) 355:743-750.
29. + channel cloned from human heart. Mol. Pharmacol. (1993) 44:642-648.
30. ZHANG X, ANDERSON JW, FEDIDA D: Characterization of nifedipine block of the human heart delayed rectifier, hKv1. 5. J. Pharmacol. Exp. Ther. (1997) 281:1247-1256.
31. VALENZUELA C, DELPON E, FRANQUEZA L et al.: Class III antiarrhythmic effects of zatebradine: time-, state-, use-, and voltage-dependent block of hKv1.5 channels. Circulation (1996) 94:562-570.
32. CHOI BK, CHOI JS, JEONG SW et al.: Direct block by bisindolylmaleimide of rat Kv1.5 expressed in chinese hamster ovary cells. J. Pharmacol. Exp. Ther. (2000) 293(2):634-640.
33. DELPON E, VALENZUELA C, GAY P, FRANQUEZA L, SNYDERS DJ, TAMARGO J: Block of human cardiac Kv1.5 channels by loratadine: voltage-, time-and use-dependent block at concentrations above therapeutic levels. Cardiovasc. Res. (1997) 35:341-350.
34. LACERDA AE, ROY ML, LEWIS EW, RAMPE D: Interactions of the nonsedating antihistamine loratadine with a Kv1.5-type potassium channel cloned from human heart. Mol. Pharmacol. (1997) 52(2):314-322.
35. YUE L, FENG J, LI GR, NATTEL S: Characterization of an ultrarapid delayed rectifier potassium channel involved in canine atrial repolarization. J. Physiol. (1996) 496:647-662
36. COGHLAN MJ, CARROLL WA, GOLAPAKRISHNAN M: Recent developments in the biology and medicinal chemistry of potassium channel modulators: update from a decade of progress. J. Med. Chem. (2001) 44(11):1-27
37. MATSUDA T, SAITO T, ITOKAWA M et al.: Atrial selective prolongation by NIP-142 of refractory period and action potential duration in guinea-pig myocardium. Jpn. J. Pharmacol. (2001) 85(Suppl.1):71.
38. NAGASAWA H, FUJIKI A, USUI M et al.: Jpn. Circ. J. (1999) 63(Suppl. 1):361P.
39. NAGASAWA H, FUJIKI A, INOUE H, FUJIKURA N: Jpn. Circ. J. (2000) 64(Suppl. 1):606P.
40. + channel Kv1.5 current. Life Sciences (2001) 68(17):2017-2024.
41. SEKI A, HAGIWARA N, KASUNAKI H: Jpn. J. Electrocardiol. (1999) 19:595P.
42. SEKI A, HAGIWARA N, KASANUKI H: Effects of NIP-141 on K-currents in human atrial myocytes. J. Cardiovasc. Pharmacol. (2002) 39:29-38.
43. NAGASAWA H, FUJIKI A, FUJIKURA N, MATSUDA T, YAMASHITA T, INOUE H: Effects of a novel class III antiarrhythmic agent, NIP-142, on canine atrial fibrillation and flutter. Circ. J. (2002) 66(2).185-191.
44. MATSUDA T, ISHIMARU S, SAITO T et al.: Effect of NIP-142 on carbachol-induced myocardial action potential shortening and human GIRK1/4 channel current. Jpn. J. Pharmacol. (2002) 88(Suppl. 1):260P.
45. SCHNEIDER G, CLEMENT-CHOMIENNE O et al.: Virtual screening for bioactive molecules by evolutionary de novo design. Angew. Chem., Int. Ed. (2000) 39:4130-4133.
46. BACHMANN A, GUTCHER I, KOPP K et al.: Characterization of a novel Kv1.5 channel blocker in Xenopus oocytes, CHO cells, human and rat cardiomyocytes. Nau. Schmied. Arch. Pharmacol. (2001) 364:472-478.
47. r blockers dofetilide, azimilide, d,l-sotalol and ibutilide. Nau. Schmied. Arch. Pharmarcol. (2002) 366:482-487.
48. TANHEHCO EJ: Potassium channel modulators as anti-inflammatory agents. Expert Opin. Ther. Patents. (2001) 11:1137-1145.
49. NO AUTHORS LISTED: Astra Zeneca company presentation, Annual Business Review Presentation, December 3rd, London, UK (2001).