Inhibition of the current of heterologously expressed HERG potassium channels by flecainide and comparison with quinidine, propafenone and lignocaine

No abstract is available for this paper.

• Publication year

  2002

• Venue

  British Journal of Pharmacology

• Publication date

  2002-07-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1038/sj.bjp.0704784PMID 12086981PMCID PMC1573407
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Comparative investigation of the antiarrhythmic effect of propafenone (Rytmonorm) and lidocaine in patients with ventricular arrhythmias during acute myocardial infarction.

  2009cited by this paper
• Inhibitory actions of the selective serotonin re‐uptake inhibitor citalopram on HERG and ventricular L‐type calcium currents

  2002cited by this paper
• Inhibition of HERG potassium channel current by the class 1a antiarrhythmic agent disopyramide.

  2001cited by this paper
• Rate dependency of delayed rectifier currents during the guinea‐pig ventricular action potential

  2001influential reference
• Open channel block of HERG K(+) channels by vesnarinone.

  2001cited by this paper
• HERG K+ channels: friend and foe.

  2001cited by this paper
• An amino acid residue whose change by mutation affects drug binding to the HERG channel

  2001cited by this paper
• Blocking effects of the antiarrhythmic drug propafenone on the HERG potassium channel

  2001influential reference
• Drug Block of I Kr : Model Systems and Relevance to Human Arrhythmias

  2001influential reference
• Comparative effects of azimilide and ambasilide on the human ether-a-go-go-related gene (HERG) potassium channel.

  2000cited by this paper
• Therapeutic drug monitoring of flecainide in serum using high-performance liquid chromatography and electrospray mass spectrometry.

  2000influential reference
• A structural basis for drug-induced long QT syndrome.

  2000cited by this paper
• Molecular determinant of high-affinity dofetilide binding to HERG1 expressed in Xenopus oocytes: involvement of S6 sites.

  2000influential reference
• Trapping of a Methanesulfonanilide by Closure of the Herg Potassium Channel Activation Gate

  2000cited by this paper
• Familial And Acquired Long QT Syndrome And The Cardiac Rapid Delayed Rectifier Potassium Current

  2000cited by this paper
• Inhibition of the current of heterologously expressed HERG potassium channels by imipramine and amitriptyline

  1999cited by this paper
• Long QT syndromes and torsade de pointes.

  1999cited by this paper
• Modulation of HERG potassium channels by extracellular magnesium and quinidine.

  1999influential reference
• Evolution, mechanisms, and classification of antiarrhythmic drugs: focus on class III actions.

  1999cited by this paper
• An investigation of the role played by the E-4031-sensitive (rapid delayed rectifier) potassium current in isolated rabbit atrioventricular nodal and ventricular myocytes

  1999cited by this paper
• Characteristics of a transient outward current (sensitive to 4-aminopyridine) in Ca2+-tolerant myocytes isolated from the rabbit atrioventricular node

  1999cited by this paper
• Properties of HERG channels stably expressed in HEK 293 cells studied at physiological temperature.

  1998influential reference
• Time course and voltage dependence of expressed HERG current compared with native ”rapid” delayed rectifier K current during the cardiac ventricular action potential

  1998cited by this paper
• Effect of disopyramide on potassium currents in rabbit ventricular myocytes

  1998influential reference
• Inhibition of L‐type calcium current by propafenone in single myocytes isolated from the rabbit atrioventricular node

  1997cited by this paper
• Electrophysiological and pharmacological correspondence between Kv4.2 current and rat cardiac transient outward current.

  1997influential reference
• Rapid inactivation determines the rectification and [K+]o dependence of the rapid component of the delayed rectifier K+ current in cardiac cells.

  1997influential reference
• Comparison of the effects of class I anti-arrhythmic drugs, cibenzoline, mexiletine and flecainide, on the delayed rectifier K+ current of guinea-pig ventricular myocytes.

  1996influential reference
• Coassembly of KVLQT1 and minK (IsK) proteins to form cardiac IKS potassium channel

  1996cited by this paper
• The inward rectification mechanism of the HERG cardiac potassium channel

  1996cited by this paper
• KvLQT1 and IsK (minK) proteins associate to form the IKS cardiac potassium current

  1996cited by this paper
• A method for making rapid changes of superfusate whilst maintaining temperature at 37 degrees C.

  1996cited by this paper
• Spectrum of HERG K+-channel dysfunction in an inherited cardiac arrhythmia.

  1996cited by this paper
• Extracellular potassium modulation of drug block of IKr. Implications for torsade de pointes and reverse use-dependence.

  1996cited by this paper
• Coassembly of K(V)LQT1 and minK (IsK) proteins to form cardiac I(Ks) potassium channel.

  1996cited by this paper
• Separation of the components of the delayed rectifier potassium current using selective blockers of IKr and IKs in guinea‐pig isolated ventricular myocytes

  1996cited by this paper
• High affinity open channel block by dofetilide of HERG expressed in a human cell line.

  1996cited by this paper
• [Sotalol, propafenone, and flecainide: compared multiparametric analysis of ventricular repolarization in subjects without organic cardiopathy].

  1996cited by this paper
• A molecular basis for cardiac arrhythmia: HERG mutations cause long QT syndrome.

  1995cited by this paper
• Propafenone preferentially blocks the rapidly activating component of delayed rectifier K+ current in guinea pig ventricular myocytes. Voltage-independent and time-dependent block of the slowly activating component.

  1995cited by this paper
• Flecainide inhibits the transient outward current in atrial myocytes isolated from the rabbit heart.

  1995influential reference
• HERG, a human inward rectifier in the voltage-gated potassium channel family.

  1995cited by this paper
• Pharmacological modulation of human cardiac Na+ channels.

  1994cited by this paper
• Flecainide

  1994cited by this paper
• Effects of propafenone on calcium currents in single ventricular myocytes of guinea‐pig

  1993influential reference
• Two delayed rectifiers in guinea pig ventricular myocytes distinguished by tail current kinetics.

  1993cited by this paper
• Mechanism of flecainide's rate-dependent actions on action potential duration in canine atrial tissue.

  1993cited by this paper
• K+channels and control of ventricular repolarization in the heart

  1993cited by this paper
• Potassium channel blocking properties of propafenone in rabbit atrial myocytes.

  1993influential reference
• Modulation of flecainide's cardiac sodium channel blocking actions by extracellular sodium: a possible cellular mechanism for the action of sodium salts in flecainide cardiotoxicity.

  1993cited by this paper
• Time-, voltage-, and state-dependent block by quinidine of a cloned human cardiac potassium channel.

  1992cited by this paper
• Differential block of cardiac delayed rectifier current by class Ic antiarrhythmic drugs: evidence for open channel block and unblock.

  1992influential reference
• Delayed rectifier outward K+ current is composed of two currents in guinea pig atrial cells.

  1991cited by this paper
• DIFFERENTIAL EFFECTS ON ACTION POTENTIAL DURATION OF CLASS IA, B AND C ANTIARRHYTHMIC DRUGS: MODULATION BY STIMULATION RATE AND EXTRACELLULAR K+ CONCENTRATION

  1991cited by this paper
• Propafenone‐Induced Torsade de Pointes: Cross‐Reactivity with Quinidine

  1991cited by this paper
• Block of delayed rectifier potassium current, IK, by flecainide and E-4031 in cat ventricular myocytes.

  1990cited by this paper
• Two components of cardiac delayed rectifier K+ current. Differential sensitivity to block by class III antiarrhythmic agents

  1990cited by this paper
• Inhibition of ICa in single frog cardiac cells by quinidine, flecainide, ethmozin, and ethacizin.

  1989cited by this paper
• [QT prolongation and induction of torsades de pointe by flecainide. Apropos of a case].

  1988cited by this paper
• Stereoselective Effects of Disopyramide Enantiomers in Humans

  1987cited by this paper
• Comparison of intravenous mexiletine and lidocaine for the treatment of ventricular arrhythmias.

  1986cited by this paper
• Kinetics of onset of rate-dependent effects of Class I antiarrhythmic drugs are important in determining their effects on refractoriness in guinea-pig ventricle, and provide a theoretical basis for their subclassification.

  1983cited by this paper
• Flecainide-induced QT prolongation and ventricular tachycardia.

  1982cited by this paper
• Characterization of a new oral antiarrhythmic drug, flecainide (R818)

  1981cited by this paper
• Steady-state serum quinidine concentration: role in prophylactic therapy following acute myocardial infarction.

  1979cited by this paper

• Repurposing of propafenone, an FDA approved anti-arrhythmic drug for antileishmanial therapy.

  2025cites this paper
• Statistical approaches to evaluate the positive control drug using the hERG assay.

  2025cites this paper
• Harnessing AlphaFold to reveal hERG channel conformational state secrets

  2025cites this paper
• Arrhythmogenic and Side Effects of Antiarrhythmic Medications.

  2025cites this paper
• Drosophila expressing mutant human KCNT1 transgenes make an effective tool for targeted drug screening in a whole animal model of KCNT1-epilepsy

  2024cites this paper
• Kir2.1 mutations differentially increase the risk of flecainide proarrhythmia in Andersen Tawil Syndrome

  2024cites this paper
• Mechanisms of Chemical Atrial Defibrillation by Flecainide and Ibutilide

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• KCNT1 Channel Blockers: A Medicinal Chemistry Perspective

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• In Silico Assisted Identification, Synthesis, and In Vitro Pharmacological Characterization of Potent and Selective Blockers of the Epilepsy-Associated KCNT1 Channel

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• Harnessing AlphaFold to reveal hERG channel conformational state secrets

  2024cites this paper
• The Antiarrhythmic Drug Flecainide Enhances Aversion to HCl in Mice

  2023cites this paper
• Modelling human KCNT1-epilepsy in Drosophila: a seizure phenotype and drug responses

  2023cites this paper
• hERG agonists pose challenges to web-based machine learning methods for prediction of drug-hERG channel interaction.

  2023cites this paper
• Comparing the effects of chemical Ca2+ dyes and R-GECO on contractility and Ca2+ transients in adult and human iPSC cardiomyocytes

  2023cites this paper
• Structural modeling of hERG channel–drug interactions using Rosetta

  2023cites this paper
• Action potential metrics and automated data analysis pipeline for cardiotoxicity testing using optically mapped hiPSC-derived 3D cardiac microtissues

  2023cites this paper
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  2022influential citation
• Molecular stratification of arrhythmogenic mechanisms in the Andersen Tawil syndrome

  2022cites this paper
• Metabolic and electrolyte abnormalities as risk factors in drug-induced long QT syndrome

  2022cites this paper
• In silico assessment of pharmacotherapy for carbon monoxide induced arrhythmias in healthy and failing human hearts

  2022cites this paper
• Increased atrial effectiveness of flecainide conferred by altered biophysical properties of sodium channels.

  2022cites this paper
• Use of automated patch clamp in cardiac safety assessment: Past, present & future perspectives.

  2021cites this paper
• Anti‐arrhythmic investigations in large animal models of atrial fibrillation

  2021cites this paper
• Cardiac hERG K+ Channel as Safety and Pharmacological Target.

  2021cites this paper
• Pharmacology of A-Type K+ Channels.

  2021cites this paper
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  2021cites this paper
• Effects of Antiarrhythmic Drugs on hERG Gating in Human-Induced Pluripotent Stem Cell-Derived Cardiomyocytes From a Patient With Short QT Syndrome Type 1

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• Computational modeling of atrial fibrillation

  2021cites this paper
• Inhibition of the hERG potassium channel by phenanthrene: a polycyclic aromatic hydrocarbon pollutant

  2021cites this paper
• hERG Channel-Related Cardiotoxicity Assessment of 13 Herbal Medicines

  2021cites this paper
• Targeting KNa1.1 channels in KCNT1-associated epilepsy.

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  2020cites this paper
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  2020influential citation
• Balance Between Rapid Delayed Rectifier K+ Current and Late Na+ Current on Ventricular Repolarization

  2020cites this paper
• KV11.1, NaV1.5, and CaV1.2 Transporter Proteins as Antitarget for Drug Cardiotoxicity

  2020cites this paper
• Clinical management of electrical storm: a current overview

  2020cites this paper
• Functional and pharmacological characterization of an S5 domain hERG mutation associated with short QT syndrome

  2019cites this paper
• Cardiac safety assessment with motion field imaging analysis of human iPS cell-derived cardiomyocytes is improved by an integrated evaluation with cardiac ion channel profiling.

  2019cites this paper
• Effects of cariprazine on hERG 1A and hERG 1A/3.1 potassium channels.

  2019cites this paper
• In silico Assessment of Pharmacotherapy for Human Atrial Patho-Electrophysiology Associated With hERG-Linked Short QT Syndrome

  2019cites this paper
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  2018cites this paper
• Measurement of myofilament calcium in living cardiomyocytes using a targeted genetically encoded indicator

  2018cites this paper
• Emerging therapeutic targets in the short QT syndrome

  2018cites this paper
• Inhibition of the voltage‐dependent K+ current by the class Ic antiarrhythmic drug flecainide in rabbit coronary arterial smooth muscle cells

  2018cites this paper
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  2018cites this paper
• Cardiac Sodium Channel (Dys)Function and Inherited Arrhythmia Syndromes

  2018cites this paper
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  2018cites this paper
• Multiple targets for flecainide action: implications for cardiac arrhythmogenesis

  2018cites this paper
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  2017cites this paper
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  2017cites this paper
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  2017cites this paper
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  2017cites this paper
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  2017cites this paper
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  2017cites this paper
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  2017cites this paper
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  2017cites this paper
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  2017cites this paper
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  2016cites this paper
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  2016cites this paper
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  2016cites this paper
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  2016cites this paper
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  2016cites this paper
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  2016cites this paper
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  2016cites this paper
• Effect of fl ecainide derivatives on sarcoplasmic reticulum calcium release suggests a lack of direct action on the cardiac ryanodine receptor Correspondence

  2016cites this paper
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  2015cites this paper
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  2015cites this paper
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  2015cites this paper
• Optimal antiarrhythmic drug therapy for electrical storm

  2015cites this paper
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  2015cites this paper
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  2015cites this paper
• Effects of donepezil on hERG potassium channels.

  2015cites this paper
• Flecainide-induced Torsades de Pointes: Case Report and Review of Literature.

  2015cites this paper
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  2015cites this paper
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  2014cites this paper
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  2014cites this paper
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  2014cites this paper
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  2014cites this paper
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  2014cites this paper
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  2014cites this paper
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  2014cites this paper
• 111 – Standard Antiarrhythmic Drugs

  2014cites this paper
• Ranolazine inhibition of hERG potassium channels: Drug–pore interactions and reduced potency against inactivation mutants

  2014cites this paper
• [To the mechanisms of antiarrhythmic action of Allapinine].

  2013cites this paper
• Enhanced prediction and prevention of drug-induced torsades de pointes

  2013cites this paper
• Diastolic Spontaneous Calcium Release From the Sarcoplasmic Reticulum Increases Beat-to-Beat Variability of Repolarization in Canine Ventricular Myocytes After &bgr;-Adrenergic Stimulation

  2013cites this paper
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  2013cites this paper
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  2013cites this paper
• Chapter 18 – Clinical Pharmacology of Antiarrhythmic Drugs

  2013cites this paper