Activation of Human ether-a-go-go-Related Gene Potassium Channels by the Diphenylurea 1,3-Bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643)

No abstract is available for this paper.

• Publication year

  2006

• Venue

  Molecular Pharmacology

• Publication date

  2006-01-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1124/mol.105.015859PMID 16219910
• 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.

• Expression of human ERG K+ channels in the mouse heart exerts anti-arrhythmic activity.

  2005cited by this paper
• Discovery of a Small Molecule Activator of the Human Ether-a-go-go-Related Gene (HERG) Cardiac K+ Channel

  2005cited by this paper
• Risperidone-induced action potential prolongation is attenuated by increased repolarization reserve due to concomitant block of ICa,L

  2005cited by this paper
• Suppression of electrical alternans by overexpression of HERG in canine ventricular myocytes.

  2004cited by this paper
• New ideas about atrial fibrillation 50 years on

  2002cited by this paper
• A comparison of currents carried by HERG, with and without coexpression of MiRP1, and the native rapid delayed rectifier current. Is MiRP1 the missing link?

  2002cited by this paper
• Dual-function vector for protein expression in both mammalian cells and Xenopus laevis oocytes.

  2002cited by this paper
• Distinct gene-specific mechanisms of arrhythmia revealed by cardiac gene transfer of two long QT disease genes, HERG and KCNE1

  2001cited by this paper
• Effects of premature stimulation on HERG K+ channels

  2001cited by this paper
• T-Type and tetrodotoxin-sensitive Ca(2+) currents coexist in guinea pig ventricular myocytes and are both blocked by mibefradil.

  2000cited by this paper
• Apamin interacts with all subtypes of cloned small-conductance Ca2+-activated K+ channels

  2000cited by this paper
• Overexpression of a human potassium channel suppresses cardiac hyperexcitability in rabbit ventricular myocytes.

  1999cited by this paper
• Pathways of HERG inactivation.

  1999cited by this paper
• MiRP1 forms IKr potassium channels with HERG and is associated with cardiac arrhythmia.

  1999cited by this paper
• Structure and function of cardiac potassium channels.

  1999cited by this paper
• Pathways of HERG inactivation.

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

  1998cited by this paper
• 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
• Acceleration‐Induced Action Potential Prolongation and Early Afterdepolarizations

  1998cited by this paper
• A minK–HERG complex regulates the cardiac potassium current IKr

  1997cited by this paper
• Facilitation of epinephrine-induced afterdepolarizations by class III antiarrhythmic drugs.

  1997cited by this paper
• Coassembly of K(V)LQT1 and minK (IsK) proteins to form cardiac I(Ks) potassium channel.

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

  1996cited by this paper
• Coassembly of KVLQT1 and minK (IsK) proteins to form cardiac IKS potassium channel

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

  1996cited by this paper
• Role of Calcium Loading in Early Afterdepolarizations Generated by Cs+ in Canine and Guinea Pig Purkinje Fibers

  1995cited by this paper
• Torsades de pointes after terfenadine-itraconazole interaction.

  1993cited by this paper
• Mechanism of the cardiotoxic actions of terfenadine.

  1993cited by this paper
• Prolongation of the Corrected QT and Torsades de Pointes Cardiac Arrhythmia Associated with Intravenous Haloperidol in the Medically III

  1993cited by this paper
• Alcohol and cor pulmonale in chronic bronchitis and emphysema.

  1993cited by this paper
• Two components of cardiac delayed rectifier K+ current. Differential sensitivity to block by class III antiarrhythmic agents

  1990cited by this paper
• Torsades de pointes occurring in association with terfenadine use.

  1990cited by this paper
• Early Afterdepolarizations: Mechanism of Induction and Block A Role for L‐Type Ca2+ Current

  1989cited by this paper
• Pharmacological response of quinidine induced early afterdepolarisations in canine cardiac Purkinje fibres: insights into underlying ionic mechanisms.

  1988cited by this paper
• A uniform enzymatic method for dissociation of myocytes from hearts and stomachs of vertebrates.

  1985cited by this paper

• Molecular Determinants of Voltage-Dependent Gating in Kv11.1 Channels.

  2026cites this paper
• Voltage-gated potassium channels (Kv) in GtoPdb v.2025.4

  2025cites this paper
• Protective function of the voltage-gated potassium channel Kv11.3 in a mouse model of cardiac ischemia/reperfusion injury

  2025influential citation
• Harnessing AlphaFold to reveal hERG channel conformational state secrets

  2025cites this paper
• Voltage-gated potassium channels (Kv) in GtoPdb v.2025.3

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

  2024cites this paper
• Drug repositioning identifies histone deacetylase inhibitors that promote innate immunity in non-tuberculous mycobacterial infection.

  2024cites this paper
• Voltage-gated potassium channels (Kv) in GtoPdb v.2023.1

  2023cites this paper
• Binding of RPR260243 at the intracellular side of the hERG1 channel pore domain slows closure of the helix bundle crossing gate

  2023influential citation
• Histone deacetylase (HDAC) inhibitors- based drugs are effective to control Mycobacterium tuberculosis infection and promote the sensibility for rifampicin in MDR strain

  2023cites this paper
• Pharmacological activation of the hERG K+ channel for the management of the long QT syndrome: A review

  2022cites this paper
• Cardiac hERG K+ Channel as Safety and Pharmacological Target.

  2021cites this paper
• Arrhythmogenic Remodeling in the Failing Heart

  2021influential citation
• Electrophysiological characterization of the hERG R56Q LQTS variant and targeted rescue by the activator RPR260243

  2021cites this paper
• Chemical modulation of Kv7 potassium channels.

  2021cites this paper
• Targeting of Potassium Channels in Cardiac Arrhythmias.

  2021cites this paper
• Heritable arrhythmias associated with abnormal function of cardiac potassium channels.

  2020cites this paper
• Optimized Tuning of Auditory Inner Hair Cells to Encode Complex Sound through Synergistic Activity of Six Independent K+ Current Entities.

  2020cites this paper
• The hERG channel activator, RPR260243, enhances protective IKr current in early refractory reducing arrhythmogenicity in zebrafish hearts.

  2020cites this paper
• LUF7244, an allosteric modulator/activator of Kv11.1 channels, counteracts dofetilide‐induced torsades de pointes arrhythmia in the chronic atrioventricular block dog model

  2019cites this paper
• Investigating the utility of adult zebrafish ex vivo whole hearts to pharmacologically screen hERG channel activator compounds.

  2019cites this paper
• Functional study of a KCNH2 mutant: Novel insights on the pathogenesis of the LQT2 syndrome

  2019cites this paper
• Electrophysiological characterization of a small molecule activator on human ether-a-go-go-related gene (hERG) potassium channel.

  2019cites this paper
• Molecular determinants of voltage sensor movement and its transduction to pore opening by the S4-S5 linker in the hERG potassium channel

  2019influential citation
• Identification and functional characterisation of potassium channels in mouse GI tract

  2019cites this paper
• 113 – Innovations in Antiarrhythmic Drug Therapy

  2018cites this paper
• Inverse Modulation of Neuronal Kv12.1 and Kv11.1 Channels by 4-Aminopyridine and NS1643

  2018cites this paper
• Manipulation-free cultures of human iPSC-derived cardiomyocytes offer a novel screening method for cardiotoxicity

  2018cites this paper
• Utility of the JT Peak Interval and the JT Area in Determining the Proarrhythmic Potential of QT-Shortening Agents

  2018cites this paper
• KV channels and the regulation of vascular smooth muscle tone

  2018cites this paper
• Discovery and electrophysiological characterization of SKF‐32802: A novel hERG agonist found through a large‐scale structural similarity search

  2018cites this paper
• Cardiac Potassium Channels: Physiological Insights for Targeted Therapy

  2017cites this paper
• First universal pharmacophore model for hERG1 K+ channel activators: acthER.

  2017cites this paper
• Trigger vs. Substrate: Multi-Dimensional Modulation of QT-Prolongation Associated Arrhythmic Dynamics by a hERG Channel Activator

  2017cites this paper
• Computational Models for Understanding of Structure, Function and Pharmacology of the Cardiac Potassium Channel Kv11.1 (hERG).

  2017cites this paper
• Murine Electrophysiological Models of Cardiac Arrhythmogenesis.

  2017cites this paper
• CSAHi study‐2: Validation of multi‐electrode array systems (MEA60/2100) for prediction of drug‐induced proarrhythmia using human iPS cell‐derived cardiomyocytes: Assessment of reference compounds and comparison with non‐clinical studies and clinical information

  2017influential citation
• Cardiac potassium channels: physiological insights for targeted therapy.

  2017cites this paper
• NS1643 enhances ionic currents in a G604S‐WT hERG co‐expression system associated with long QT syndrome 2

  2017cites this paper
• Kinetic Image Cytometry for Predicting Arrhythmias Using Human Stem Cell-Derived Cardiomyocytes

  2017cites this paper
• Proliferative Role of Kv11 Channels in Murine Arteries

  2017cites this paper
• Modulation of Kv11.1 (hERG) channels by 5‐(((1H–indazol‐5‐yl)oxy)methyl)‐N‐(4‐(trifluoromethoxy)phenyl)pyrimidin‐2‐amine (ITP‐2), a novel small molecule activator

  2017influential citation
• Application of optical action potentials in human induced pluripotent stem cells-derived cardiomyocytes to predict drug-induced cardiac arrhythmias.

  2017cites this paper
• Molecular Pathophysiology of Congenital Long QT Syndrome.

  2017cites this paper
• Dissociative States: hERG Channel (Kv11.1) Modulators That Enhance Dissociation of Drugs From Their Blocking Receptor: Potential New Therapeutic Drugs.

  2016cites this paper
• A dual potassium channel activator improves repolarization reserve and normalizes ventricular action potentials.

  2016cites this paper
• Molecular Basis of Cardiac Delayed Rectifier Potassium Channel Function and Pharmacology.

  2016cites this paper
• Molecular Basis of Cardiac Delayed Rectifier K + Channel Function and Pharmacology

  2016cites this paper
• Assessment of drug-induced proarrhythmia: The importance of study design in the rabbit left ventricular wedge model.

  2016cites this paper
• Human iPS cell models of Jervell and Lange-Nielsen syndrome

  2015cites this paper
• Activation of HERG channels: opening new applications for the biophysics of antiarrhythmic therapy.

  2015cites this paper
• Pharmacological and electrophysiological characterization of AZSMO‐23, an activator of the hERG K+ channel

  2015influential citation
• A ligand-based virtual screening approach to identify small molecules as HERG channel activators.

  2015cites this paper
• Kinetic model for NS1643 drug activation of WT and L529I variants of Kv11.1 (hERG1) potassium channel.

  2015cites this paper
• The Human Ether-A-Go-Go–Related Gene Activator NS1643 Enhances Epilepsy-Associated KCNQ Channels

  2014cites this paper
• 112 – New Antiarrhythmic Drugs and New Concepts for Old Drugs

  2014cites this paper
• Cardiac potassium channel subtypes: new roles in repolarization and arrhythmia.

  2014cites this paper
• Recessive cardiac phenotypes in induced pluripotent stem cell models of Jervell and Lange-Nielsen syndrome: Disease mechanisms and pharmacological rescue

  2014cites this paper
• Future perspectives in the pharmacological treatment of atrial fibrillation and ventricular arrhythmias in heart failure.

  2014cites this paper
• Stoichiometry of altered hERG1 channel gating by small molecule activators

  2014cites this paper
• Potassium channel activation inhibits proliferation of breast cancer cells by activating a senescence program

  2013cites this paper
• Halide Ion Effects on Human Ether-à-go-go Related Gene Potassium Channel Properties

  2013cites this paper
• Compound ICA-105574 prevents arrhythmias induced by cardiac delayed repolarization.

  2013influential citation
• Repolarization reserve, arrhythmia and new drug development

  2013cites this paper
• ICA-105574 Interacts with a Common Binding Site to Elicit Opposite Effects on Inactivation Gating of EAG and ERG Potassium Channels

  2013cites this paper
• Effects of an hERG activator, ICA-105574, on electrophysiological properties of canine hearts.

  2013cites this paper
• A history of the role of the hERG channel in cardiac risk assessment.

  2013cites this paper
• Characterization of A-935142, a hERG enhancer, in the presence and absence of standard hERG blockers.

  2012cites this paper
• K(+) channels: function-structural overview.

  2012cites this paper
• High throughput measurement of Ca²⁺ dynamics for drug risk assessment in human stem cell-derived cardiomyocytes by kinetic image cytometry.

  2012cites this paper
• hERG K(+) channels: structure, function, and clinical significance.

  2012cites this paper
• Effects of the Small Molecule HERG Activator NS1643 on Kv11.3 Channels

  2012cites this paper
• Modulation of hERG potassium channel gating normalizes action potential duration prolonged by dysfunctional KCNQ1 potassium channel

  2012cites this paper
• Title Pharmacology of Cardiac Potassium Channels

  2011cites this paper
• Molecular Determinants for Activation of Human Ether-à-go-go-related Gene 1 Potassium Channels by 3-Nitro-N-(4-phenoxyphenyl) Benzamide

  2011cites this paper
• Enhanced repolarization capacity: new potential antiarrhythmic strategy based on HERG channel activation.

  2011cites this paper
• Cardiac models in drug discovery and development: a review.

  2011cites this paper
• Ginsenoside Rg(3) decelerates hERG K(+) channel deactivation through Ser631 residue interaction.

  2011cites this paper
• Molecular Determinants of Human ether-à-go-go-Related Gene 1 (hERG1) K+ Channel Activation by NS1643

  2011cites this paper
• Regulation and physiological function of Nav1.5 and KCNQ1 channels

  2011cites this paper
• Pharmacological Activation of Kv11.1 in Transgenic Long QT-1 Rabbits

  2011cites this paper
• (1,3-bis-(2-hydroxy-5-trifluoromethylphenyl)-urea) in HEK-293 and CHO cells

  2011influential citation
• hERG Potassium Channels in Drug Discovery and Development

  2011cites this paper
• hERG1 Channel Blockers and Cardiac Arrhythmia

  2011cites this paper
• Strong Activation of ether-à-go-go-Related Gene 1 K+ Channel Isoforms by NS1643 in Human Embryonic Kidney 293 and Chinese Hamster Ovary Cells

  2011influential citation
• Cardiac ventricular repolarization reserve: a principle for understanding drug‐related proarrhythmic risk

  2011cites this paper
• Repolarization of the cardiac action potential. Does an increase in repolarization capacity constitute a new anti‐arrhythmic principle?

  2010cites this paper
• QTc shortening with a new investigational cancer drug: a brief case study.

  2010cites this paper
• Rescue of mutated cardiac ion channels in inherited arrhythmia syndromes.

  2010cites this paper
• Synthesis and characterisation of NS13558: a new important tool for addressing KCa1.1 channel function ex vivo

  2010cites this paper
• The Novel Mechanism of Oxymatrine Affecting hERG Currents at Different Temperatures

  2010cites this paper
• Minimizing Repolarization-Related Proarrhythmic Risk in Drug Development and Clinical Practice

  2010cites this paper
• Pharmacological Removal of Human Ether-à-go-go-Related Gene Potassium Channel Inactivation by 3-Nitro-N-(4-phenoxyphenyl) Benzamide (ICA-105574)

  2010influential citation
• Pharmacology of cardiac potassium channels.

  2010cites this paper
• Pharmacological modulation of voltage-gated potassium channels as a therapeutic strategy

  2010cites this paper
• The amiodarone derivative KB130015 activates hERG1 potassium channels via a novel mechanism.

  2010cites this paper
• Pharmacological Activation of IKr Impairs Conduction in Guinea Pig Hearts

  2010cites this paper
• Differential effects of Kv11.1 activators on Kv11.1a, Kv11.1b and Kv11.1a/Kv11.1b channels

  2010cites this paper
• Drug induced shortening of the QT/QTc interval: an emerging safety issue warranting further modelling and evaluation in drug research and development?

  2009cites this paper
• Pharmacologically Induced Long QT Type 2 Can Be Rescued by Activation of IKs With Benzodiazepine R-L3 in Isolated Guinea Pig Cardiomyocytes

  2009cites this paper