Kv1.5 open channel block by the antiarrhythmic drug disopyramide: Molecular determinants of block

Journal of Pharmacological Sciences

Volumn 108, Issue 1, 2008, Pages 49-55

  Aréchiga, Iván A ^a   Barrio Echavarria, Gabriel F ^a   Rodríguez Menchaca, Aldo A ^a   Moreno Galindo, Eloy G ^a   Decher, Niels ^b   Tristani Firouzi, Martin ^c   Sánchez Chapula, José A ^a   Navarro Polanco, Ricardo A ^a  

^a Universidad de Colima   (Mexico)

^b PHILIPPS UNIVERSITY MARBURG   (Germany)

^c UNIVERSITY OF UTAH SCHOOL OF MEDICINE   (United States)

Author keywords

Antiarrhythmic; Disopyramide; Kv1.5; Potassium channel; Ultra rapid delayed rectifier

Indexed keywords

2' (4 METHOXYPHENYLACETAMIDOMETHYL) N [2 (3 PYRIDYL)ETHYL] 2 BIPHENYLCARBOXAMIDE; DISOPYRAMIDE; ICAGEN 4; POTASSIUM CHANNEL BLOCKING AGENT; POTASSIUM CHANNEL KV1.5; POTASSIUM CHANNEL KV1.5 BLOCKING AGENT; S 0100176; S 9947; UNCLASSIFIED DRUG; VALINE; VERNAKALANT;

ALANINE SCANNING MUTAGENESIS; ANALYTIC METHOD; ARTICLE; BINDING SITE; CONTROLLED STUDY; DRUG MECHANISM; FOOT IN THE DOOR PHENOMENON; HEART ARRHYTHMIA; HEART ATRIUM FIBRILLATION; HEART ATRIUM FLUTTER; HUMAN; HUMAN CELL; IC 50; PATCH CLAMP; PHENOMENOLOGY; POTASSIUM CURRENT; PROTEIN DOMAIN; SITE DIRECTED MUTAGENESIS; WILD TYPE;

EID: 52949138206     PISSN: 13478613     EISSN: 13478648     Source Type: Journal    
DOI: 10.1254/jphs.08084FP     Document Type: Article

References (45)

1. Choudhury A, Lip GY. Antiarrhythmic drugs in atrial fibrillation: an overview of new agents, their mechanisms of action and potential clinical utility. Expert Opin Invest Drugs. 2004;13: 841-855.
2. + current similar to Kv1.5 cloned channel currents. Circ Res. 1993;73:1061-1076.
3. + channel current. Circ Res. 1993;73:210-216.
4. Snyders D, Tamkun M, Bennett P. A rapidly activating and slowly inactivating potassium channel cloned from human heart. Functional analysis after stable mammalian cell culture expression. J Gen Physiol. 1993;101:513-543.
5. Goldstein RN, Khrestian C, Carlsson L, Waldo AL. Azd7009: a new antiarrhythmic drug with predominant effects on the atria effectively terminates and prevents reinduction of atrial fibrillation and flutter in the sterile pericarditis model. J Cardiovasc Electrophysiol. 2004;15:1444-1450.
6. Blaauw Y, Gogelein H, Tieleman RG, van Hunnik A, Schotten U, Allessie MA. "Early" class III drugs for the treatment of atrial fibrillation: efficacy and atrial selectivity of AVE0118 in remodeled atria of the goat. Circulation. 2004;110:1717-1724.
7. Wettwer E, Hala O, Christ T, Heubach JF, Dobrev D, Knaut M, et al. Role of IKur in controlling action potential shape and contractility in the human atrium: influence of chronic atrial fibrillation. Circulation. 2004;110:2299-2306.
8. Camm AJ, Savalieva I. Advances in antiarrhythmic drug treatment of atrial fibrillation: where do we stand now? Heart Rhythm. 2004;1:244-246.
9. Roden D. Antiarrhythmic drugs. In: Hardman JG, Limbird L editors. Goodman & Gilman's: The Pharmacological Basis of Therapeutics. 10th ed. New York: McGraw-Hill; 2002. p. 933-979.
10. + current by disopyramide and lidocaine in guinea pig ventricular myocytes. Circ Res. 1991;68:653-661.
11. Koumi S, Sato R, Hisatome I, Hayakawa H, Okumura H, Katori R. Disopyramide block of cardiac sodium current after removal of the fast inactivation process in guinea pig ventricular myocytes. J Pharmacol Exp Ther. 1992;261:1167-1174.
12. Grant AO, Wendt DJ, Zilberter Y, Starmer CF. Kinetics of interaction of disopyramide with the cardiac sodium channel: fast dissociation from open channels at normal rest potentials. J Membr Biol. 1993;136:199-214.
13. + current in rabbit ventricular myocytes. Cardiovasc Drugs Ther. 1993;7 Suppl 3:599-604.
14. Virag L, Varro A, Papp JG. Effect of disopyramide on potassium currents in rabbit ventricular myocytes. Naunyn Schmiedebergs Arch Pharmacol. 1998;357:268-275.
15. + channel block by disopyramide. J Pharmacol Exp Ther. 1999;290:515-523.
16. Paul AA, Witchel HJ, Hancox JC. Inhibition of HERG potassium channel current by the class 1a antiarrhythmic agent disopyramide. Biochem Biophys Res Commun. 2001;9:1243-1250.
17. + channel. J Cardiovasc Pharmacol. 1999;32:521-526.
18. + channel. Role of S6 in anti-arrhythmic drug binding. Circ Res. 1996;78:1105-1114.
19. + channels. J Biol Chem. 2004;279:394-400.
20. Decher N, Kumar P, Gonzalez T, Pirard B, Sanguinetti MC. Binding site of a novel Kv1.5 blocker: a "foot in the door" against atrial fibrillation. Mol Pharmacol. 2006;70:1204-1211.
21. Mirro MJ, Manalan AS, Bailey JC, Watanabe AM. Anticholinergic effects of disopyramide and quinidine on guinea pig myocardium. Mediation by direct muscarinic receptor blockade. Circ Res. 1980;47:855-865.
22. Nakajima T, Kurachi Y, Ito H, Takikawa R, Sugimoto T. Anticholinergic effects of quinidine, disopyramide, and procainamide in isolated atrial myocytes: mediation by different molecular mechanisms. Circ Res. 1989;64:297-303.
23. Sunami A, Fan Z, Nitta J, Hiraoka M. Two components of use-dependent block of Na+ current by disopyramide and lidocaine in guinea pig ventricular myocytes. Circ Res. 1991;68:653-661.
24. Koumi S, Sato R, Hisatome I, Hayakawa H, Okumura H, Katori R. Disopyramide block of cardiac sodium current after removal of the fast inactivation process in guinea pig ventricular myocytes. J Pharmacol Exp Ther. 1992;261:1167-1174.
25. Snyders DJ, Knoth KM, Roberds SL, Tamkun MM. Time-, voltage-, and state-dependent block by quinidine of a cloned human cardiac potassium channel. Mol Pharmacol. 1992;41: 322-330.
26. Armstrong CM. Interaction of tetraethylammonium ion derivatives with the potassium channels of giant axons. J Gen Physiol. 1971:58:413-437.
27. Nakamura M, Xue Y, Eto K, Hashimoto K. Antiarrhythmic effects of optical isomers of disopyramide on canine ventricular arrhythmias. J Cardiovasc Pharmacol. 1996;27:368-375.
28. + channels. Proc Natl Acad Sci U S A. 1996;93:13357-13361.
29. Hockerman GH, Johnson BD, Scheuer T, Catterall WA. Molecular determinants of high affinity phenylalkylamine block of L-type calcium channels. J Biol Chem. 1995;270:22119-22122.
30. 2+ channel. Proc Natl Acad Sci U S A. 1997;94:14906-14911.
31. Ragsdale DS, McPhee JC, Scheuer T, Catterall WA. Common molecular determinants of local anesthetic, antiarrhythmic, and anticonvulsant block of voltage-gated Na+ channels. Proc Natl Acad Sci U S A. 1996;93:9270-9275.
32. Peterson BZ, Johnson BD, Hockerman GH, Acheson M, Scheuer T, Catterall WA. Analysis of the dihydropyridine receptor site of L-type calcium channels by alanine-scanning mutagenesis. J Biol Chem. 1997;272:18752-18758.
33. Mitcheson JS, Chen J, Lin M, Culberson C, Sanguinetti MC. A structural basis for drug-induced long QT syndrome. Proc Natl Acad Sci U S A. 2000;97:12329-12333.
34. Snyders J, Yeola SW. Determinants of antiarrhythmic drug action. Electrostatic and hydrophobic components of block of the human cardiac hKv1.5 channel. Circ Res. 1995;77:575-583.
35. Franqueza L, Longobardo M, Vicente J, Delpon E, Tamkun MM, Tamargo J, et al. Molecular determinants of stereoselective bupivacaine block of hKv1.5 channels. Circ Res. 1997;81:1053-1064.
36. Valenzuela C, Delpon E, Tamkun MM, Tamargo J, Snyders DJ. Stereoselective block of a human cardiac potassium channel (Kv1.5) by bupivacaine enantiomers. Biophys J. 1995;69:418-427.
37. Caballero R, Moreno I, Gonzalez T, Valenzuela C, Tamargo J, Delpon E. Putative binding sites for benzocaine on a human cardiac cloned channel (Kv1.5). Cardiovasc Res. 2002;56:104-117.
38. Long SB, Campbell EB, MacKinnon R. Crystal structure of a mammalian voltage-dependent shaker family K+ channel. Science. 2005;309:897-903.
39. Strutz-Seebohm N, Gutcher I, Decher N, Steinmeyer K, Lang F, Seebohm G. Comparison of potent Kv1.5 potassium channel inhibitors reveals the molecular basis for blocking kinetics and binding mode. Cell Physiol Biochem. 2007;20:791-800.
40. Eldstrom J, Wang Z, Xu H, Pourrier M, Ezrin A, Gibson K, et al. The molecular basis of high-affinity binding of the antiarrhythmic compound vernakalant (RSD1235) to Kv1.5 channels. Mol Pharmacol. 2007;72:1522-1534.
41. Kamiya K, Niwa R, Mitcheson JS, Sanguinetti MC. Molecular determinants of HERG channel block. Mol Pharmacol. 2006;69:1709-1716.
42. Witchel HJ, Dempsey CE, Sessions RB, Perry M, Milnes JT, Hancox JC, et al. The low-potency, voltage-dependent HERG blocker propafenone-molecular determinants and drug trapping. Mol Pharmacol. 2004;66:1201-1212.
43. Ridley JM, Dooley PC, Milnes JT, Witchel HJ, Hancox JC. Lidoflazine is a high affinity blocker of the HERG K(+)channel. J Mol Cell Cardiol. 2004;36:701-705.
44. Duncan RS, Ridley JM, Dempsey CE, Leishman DJ, Leaney JL, Hancox JC, et al. Erythromycin block of the HERG K+ channel: accessibility to F656 and Y652. Biochem Biophys Res Commun. 2006;341:500-506.
45. Ferrer-Villada T, Navarro-Polanco RA, Rodriguez-Menchaca AA, Benavides-Haro DE, Sanchez-Chapula JA. Inhibition of cardiac HERG potassium channels by antidepressant mapro-tiline. Eur J Pharmacol. 2006;531:1-8.