ArticleBritish journal of pharmacology2006
Comparison of HERG channel blocking effects of various beta-blockers-- implication for clinical strategy.
Article in British journal of pharmacology, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
18 citing papers in PubMed, 45 citations in OpenAlex.
- A hERG Blocker Facilitates KbioRxiv : the preprint server for biology · 2026Article
- Systematic evaluation of Tox21 compounds that target β-adrenergic receptors and their role in cardiotoxicity.Toxicology and applied pharmacology · 2025Article
- Editorial: Repurposing β-blockers for non-cardiovascular diseases.Frontiers in pharmacology · 2024Article
- Differential Effects of the Betablockers Carvedilol, Metoprolol and Bisoprolol on Cardiac KInternational journal of molecular sciences · 2023Article
- The Potential Mechanisms behind Loperamide-Induced Cardiac Arrhythmias Associated with Human Abuse and Extreme Overdose.Biomolecules · 2023Article
- Calculations of the binding free energies of the ComprehensiveBiophysics and physicobiology · 2023Article
- Article
- Effects of Calcium, Magnesium, and Potassium Concentrations on Ventricular Repolarization in Unselected Individuals.Journal of the American College of Cardiology · 2019Article
- Usefulness of Bnet, a Simple Linear Metric in Discerning Torsades De Pointes Risks in 28 CiPA Drugs.Frontiers in pharmacology · 2019Article
- International Multisite Study of Human-Induced Pluripotent Stem Cell-Derived Cardiomyocytes for Drug Proarrhythmic Potential Assessment.Cell reports · 2018Article
- Control of the heart rate of rat embryos during the organogenic period.Hypoxia (Auckland, N.Z.) · 2016Article
- Genetics of inherited primary arrhythmia disorders.The application of clinical genetics · 2015Review
- Modulation of K2P 2.1 and K2P 10.1 K(+) channel sensitivity to carvedilol by alternative mRNA translation initiation.British journal of pharmacology · 2014Article
- Functional cross-talk between the α1- and β1-adrenergic receptors modulates the rapidly activating delayed rectifier potassium current in guinea pig ventricular myocytes.International journal of molecular sciences · 2014Article
- Field and action potential recordings in heart slices: correlation with established in vitro and in vivo models.British journal of pharmacology · 2012Article
- Predicting the potency of hERG K⁺ channel inhibition by combining 3D-QSAR pharmacophore and 2D-QSAR models.Journal of molecular modeling · 2012Article
- Carvedilol targets human K2P 3.1 (TASK1) K+ leak channels.British journal of pharmacology · 2011Article
- Filamin C: a novel component of the KCNE2 interactome during hypoxia.Cardiovascular journal of AfricaArticle
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
beta-Blockers are widely used in the treatment of cardiovascular diseases. However, their effects on HERG channels at comparable conditions remain to be defined. We investigated the direct acute effects of beta-blockers on HERG current and the molecular basis of drug binding to HERG channels with mutations of putative common binding site (Y652A and F656C). beta-Blockers were selected based on the receptor subtype. Wild-type, Y652A and F656C mutants of HERG channel were stably expressed in HEK293 cells, and the current was recorded by using whole-cell patch-clamp technique (23 degrees C). Carvedilol (nonselective), propranolol (nonselective) and ICI 118551 (beta(2)-selective) inhibited HERG current in a concentration-dependent manner (IC(50) 0.51, 3.9 and 9.2 microM, respectively). The IC(50) value for carvedilol was a clinically relevant concentration. High metoprolol (beta(1)-selective) concentrations were required for blockade (IC(50) 145 microM), and atenolol (beta(1)-selective) did not inhibit the HERG current. Inhibition of HERG current by carvedilol, propranolol and ICI 118551 was partially but significantly attenuated in Y652A and F656C mutant channels. Affinities of metoprolol to Y652A and F656C mutant channels were not different compared with the wild-type. HERG current block by all beta-blockers was not frequency-dependent. Drug affinities to HERG channels were different in beta-blockers. Our results provide additional strategies for clinical usage of beta-blockers. Atenolol and metoprolol may be preferable for patients with type 1 and 2 long QT syndrome. Carvedilol has a class III antiarrhythmic effect, which may provide the rationale for a favourable clinical outcome compared with other beta-blockers as suggested in the recent COMET (Carvedilol Or Metoprolol European Trial) substudy.
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