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Characterization of hERG K+ channel inhibition by the new class III antiarrhythmic drug cavutilide
Cavutilide (niferidil, refralon) is a new class III antiarrhythmic drug which effectively terminates persistent atrial fibrillation (AF; 84.6% of...
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Cell-Based hERG Channel Inhibition Assay in High-Throughput Format
Human ether-a-go-go-related gene (hERG) channel plays an essential role in the repolarization of the cardiac action potential. Genetic mutations and...
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Cardiac hERG K+ Channel as Safety and Pharmacological Target
The human ether-á-go-go related gene (hERG, KCNH2) encodes the pore-forming subunit of the potassium channel responsible for a fast component of the...
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A novel mutation in KCNH2 yields loss-of-function of hERG potassium channel in long QT syndrome 2
Mutations in hERG (human ether-à-go-go-related gene) potassium channel are closely associated with long QT syndromes. By direct Sanger sequencing, we...
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Systematical Evaluation of the Structure-Cardiotoxicity Relationship of 7-Azaindazole-based PI3K Inhibitors Designed by Bioisosteric Approach
A growing concern of cardiotoxicity induced by PI3K inhibitors has raised the requirements to evaluate the structure-cardiotoxicity relationship...
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Cardiovascular Safety Assessment of New Chemical Entities: Current Perspective and Emerging Technologies
The origin of cardiovascular (CVS) safety assessment studies was marked with the constitution of ICH guidelines that govern the majority of...
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Web Services for the Prediction of ADMET Parameters Relevant to the Design of Neuroprotective Drugs
The ADMET properties (absorption, distribution, metabolism, excretion, and toxicity) of a compound are key factors in its success as a drug. While...
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Antipsychotics and risk of QT prolongation: a pharmacovigilance study
RationaleWhile meta-analyses of clinical trials found that lurasidone and partial dopamine agonists (brexpiprazole and aripiprazole) were the...
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The grapefruit polyphenol naringenin inhibits multiple cardiac ion channels
Drinking fresh grapefruit juice is associated with a significant prolongation of the QT segment on the electrocardiogram (ECG) in healthy volunteers....
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Zebrafish cardiac repolarization does not functionally depend on the expression of the hERG1b-like transcript
Zebrafish provide a translational model of human cardiac function. Their similar cardiac electrophysiology enables screening of human cardiac...
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The pyridazine heterocycle in molecular recognition and drug discovery
The pyridazine ring is endowed with unique physicochemical properties, characterized by weak basicity, a high dipole moment that subtends π-π...
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The atypic antipsychotic clozapine inhibits multiple cardiac ion channels
Clozapine is an atypical neuroleptic used to manage treatment-resistant schizophrenia which is known to inhibit cardiac hERG/K V 11.1 potassium...
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Unraveling the Pharmaceutical Benefits of Freshly Prepared Amino Acid-Based Schiff Bases Via DFT, In Silico Molecular Docking and ADMET
A series of amino acid-based Schiff bases have been synthesized using a facile condensation between benzil (a diketone) and amino acid in the...
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Artificial Intelligence in Drug Safety and Metabolism
The use of artificial intelligence methods in drug safety began in the early 2000s with applications such as predicting bacterial mutagenicity and...
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Parent and Metabolite Concentration-QT Modeling to Evaluate QT-Interval Prolongation at Savolitinib Therapeutic Doses
Savolitinib is an oral, potent, and highly selective MET-tyrosine kinase inhibitor under investigation in various tumor types. A thorough QT study...
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Antimalarial activity assay of artesunate-3-chloro-4(4-chlorophenoxy) aniline in vitro and in mice models
The global spread of multi-drug resistant P. falciparum , P. vivax , and P. malariae strains and absence of long-term effective vaccine makes...
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Therapeutic Targeting of Potassium Channels
Potassium (K+) channels are the largest group of ion channels in mammals. The immediate function of these channels is electrogenic transport of K+...
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Detection of a novel pathogenic variant in KCNH2 associated with long QT syndrome 2 using whole exome sequencing
BackgroundLong QT syndrome (LQTS) is a cardiac channelopathy characterized by impaired myocardial repolarization that predisposes to life-threatening...
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Opioids-Induced Long QT Syndrome: A Challenge to Cardiac Health
The challenge posed by opioid overdose has become a significant concern for health systems due to the complexities associated with drug prohibition,...
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The Short QT Syndrome
The short QT syndrome (SQTS) is characterised by abbreviated QT intervals on the electrocardiogram and by an increased risk of atrial and ventricular...