Literature DB >> 14985067

In vivo electrophysiological effects of a selective slow delayed-rectifier potassium channel blocker in anesthetized dogs: potential insights into class III actions.

Hideko Nakashima1, Uwe Gerlach, Dietmar Schmidt, Stanley Nattel.   

Abstract

OBJECTIVES: This study evaluated the in vivo electrophysiological effects of a highly selective slow delayed-rectifier K+-current blocker, HMR 1556, to gain insights into the consequences of selectively inhibiting the slow delayed-rectifier current in vivo.
METHODS: Atrial and ventricular effective refractory periods, sinus node recovery time, Wenckebach cycle-length, atrial fibrillation duration and electrocardiographic intervals were measured before and after intravenous HMR 1556.
RESULTS: HMR 1556 increased atrial and ventricular refractory periods (e.g. by 6 +/- 4% and 27 +/- 6% at cycle lengths of 360 and 400 ms, respectively), QT intervals and sinus-node recovery times. Beta-adrenoceptor blockade with nadolol abolished all effects except those on ventricular refractoriness and changed positive use-dependent effects on refractoriness to reverse use-dependent ones. In the presence of dofetilide to block rapid delayed-rectifier current, HMR 1556 effects were potentiated (e.g. atrial and ventricular refractory periods increased by 26 +/- 3% and 34 +/- 3% at cycle lengths of 360 and 400 ms, respectively). HMR 1556 reduced vagal atrial fibrillation duration from 1077 +/- 81 to 471 +/- 38 s, an effect abolished by nadolol and greatly potentiated by dofetilide (duration 77 +/- 30 s). HMR 1556 increased Wenckebach cycle length only in the presence of dofetilide.
CONCLUSIONS: Slowed delayed-rectifier current inhibition affects atrial repolarization, sinus node function and atrial fibrillation in vivo, but only in the presence of intact beta-adrenergic tone, and delays ventricular repolarization even when beta-adrenoceptors are blocked. The slow delayed-rectifier current is particularly important when rapid delayed-rectifier current is suppressed, illustrating the importance of repolarization reserve.

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Year:  2004        PMID: 14985067     DOI: 10.1016/j.cardiores.2003.12.016

Source DB:  PubMed          Journal:  Cardiovasc Res        ISSN: 0008-6363            Impact factor:   10.787


  11 in total

Review 1.  Slow delayed rectifier potassium current (IKs) and the repolarization reserve.

Authors:  Norbert Jost; Julius Gy Papp; András Varró
Journal:  Ann Noninvasive Electrocardiol       Date:  2007-01       Impact factor: 1.468

2.  Blockade of IKs by HMR 1556 increases the reverse rate-dependence of refractoriness prolongation by dofetilide in isolated rabbit ventricles.

Authors:  Petsy Pui-Sze So; Xu-Dong Hu; Peter H Backx; José Luis Puglisi; Paul Dorian
Journal:  Br J Pharmacol       Date:  2006-06       Impact factor: 8.739

3.  Selective targeting of gain-of-function KCNQ1 mutations predisposing to atrial fibrillation.

Authors:  Courtney M Campbell; Jonathan D Campbell; Christopher H Thompson; Eleonora Savio Galimberti; Dawood Darbar; Carlos G Vanoye; Alfred L George
Journal:  Circ Arrhythm Electrophysiol       Date:  2013-09-04

Review 4.  Mechanisms of termination and prevention of atrial fibrillation by drug therapy.

Authors:  A J Workman; G L Smith; A C Rankin
Journal:  Pharmacol Ther       Date:  2011-02-18       Impact factor: 12.310

5.  Contribution of I Ks to ventricular repolarization in canine myocytes.

Authors:  Balázs Horváth; János Magyar; Norbert Szentandrássy; Péter Birinyi; Péter P Nánási; Tamás Bányász
Journal:  Pflugers Arch       Date:  2006-04-04       Impact factor: 3.657

Review 6.  Voltage-gated potassium channels as therapeutic targets.

Authors:  Heike Wulff; Neil A Castle; Luis A Pardo
Journal:  Nat Rev Drug Discov       Date:  2009-12       Impact factor: 84.694

7.  Atrial-selective effects of chronic amiodarone in the management of atrial fibrillation.

Authors:  Alexander Burashnikov; José M Di Diego; Serge Sicouri; Marcela Ferreiro; Leif Carlsson; Charles Antzelevitch
Journal:  Heart Rhythm       Date:  2008-09-16       Impact factor: 6.343

8.  Gene-specific effect of beta-adrenergic blockade on corrected QT interval in the long QT syndrome.

Authors:  Fabrice Extramiana; Pierre Maison-Blanche; Isabelle Denjoy; Patrick De Jode; Anne Messali; Jean-Philippe Labbé; Antoine Leenhardt
Journal:  Ann Noninvasive Electrocardiol       Date:  2013-05-03       Impact factor: 1.468

9.  Potentiation of E-4031-induced torsade de pointes by HMR1556 or ATX-II is not predicted by action potential short-term variability or triangulation.

Authors:  G Michael; J Dempster; K A Kane; S J Coker
Journal:  Br J Pharmacol       Date:  2007-10-29       Impact factor: 8.739

10.  Slow delayed rectifier K+ current block by HMR 1556 increases dispersion of repolarization and promotes Torsades de Pointes in rabbit ventricles.

Authors:  P P-S So; P H Backx; P Dorian
Journal:  Br J Pharmacol       Date:  2008-10-06       Impact factor: 8.739

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