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Status: Bibliographieeintrag

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Verfasst von:Rahm, Ann-Kathrin [VerfasserIn]   i
 Hackbarth, Juline [VerfasserIn]   i
 Müller, Mara Elena [VerfasserIn]   i
 Pfeiffer, Julia [VerfasserIn]   i
 Gampp, Heike [VerfasserIn]   i
 Petersenn, Finn [VerfasserIn]   i
 Rivinius, Rasmus [VerfasserIn]   i
 Frey, Norbert [VerfasserIn]   i
 Lugenbiel, Patrick [VerfasserIn]   i
 Thomas, Dierk [VerfasserIn]   i
Titel:Differential effects of the Betablockers Carvedilol, Metoprolol and Bisoprolol on cardiac Kv4.3 (Ito) channel isoforms
Verf.angabe:Ann-Kathrin Rahm, Juline Hackbarth, Mara E. Müller, Julia Pfeiffer, Heike Gampp, Finn Petersenn, Rasmus Rivinius, Norbert Frey, Patrick Lugenbiel and Dierk Thomas
Jahr:2023
Umfang:16 S.
Illustrationen:Illustrationen
Fussnoten:Veröffentlicht: 8. September 2023 ; Gesehen am 21.11.2023 ; Im Titel sind der Buchstabe "v" und der Ausdruck "to" tiefgestellt
Titel Quelle:Enthalten in: International journal of molecular sciences
Ort Quelle:Basel : Molecular Diversity Preservation International, 2000
Jahr Quelle:2023
Band/Heft Quelle:24(2023), 18, Artikel-ID 13842, Seite 1-16
ISSN Quelle:1422-0067
 1661-6596
Abstract:Cardiac Kv4.3 channels contribute to the transient outward K+ current, Ito, during early repolarization of the cardiac action potential. Two different isoforms of Kv4.3 are present in the human ventricle and exhibit differential remodeling in heart failure (HF). Cardioselective betablockers are a cornerstone of HF with reduced ejection fraction therapy as well as ventricular arrhythmia treatment. In this study we examined pharmacological effects of betablockers on both Kv4.3 isoforms to explore their potential for isoform-specific therapy. Kv4.3 isoforms were expressed in Xenopus laevis oocytes and incubated with the respective betablockers. Dose-dependency and biophysical characteristics were examined. HEK 293T-cells were transfected with the two Kv4.3 isoforms and analyzed with Western blots. Carvedilol (100 µM) blocked Kv4.3 L by 77 ± 2% and Kv4.3 S by 67 ± 6%, respectively. Metoprolol (100 µM) was less effective with inhibition of 37 ± 3% (Kv4.3 L) and 35 ± 4% (Kv4.3 S). Bisoprolol showed no inhibitory effect. Current reduction was not caused by changes in Kv4.3 protein expression. Carvedilol inhibited Kv4.3 channels at physiologically relevant concentrations, affecting both isoforms. Metoprolol showed a weaker blocking effect and bisoprolol did not exert an effect on Kv4.3. Blockade of repolarizing Kv4.3 channels by carvedilol and metoprolol extend their pharmacological mechanism of action, potentially contributing beneficial antiarrhythmic effects in normal and failing hearts.
DOI:doi:10.3390/ijms241813842
URL:Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.

kostenfrei: Volltext: https://doi.org/10.3390/ijms241813842
 kostenfrei: Volltext: https://www.mdpi.com/1422-0067/24/18/13842
 DOI: https://doi.org/10.3390/ijms241813842
Datenträger:Online-Ressource
Sprache:eng
Sach-SW:antiarrhythmic effects
 betablocker
 heart failure
 Ito
 Kv4.3
K10plus-PPN:187074523X
Verknüpfungen:→ Zeitschrift

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