Results 171 to 180 of about 1,218,415 (224)

Synthetic cannabinoid receptor agonists inhibit the cardiac voltage-gated potassium channel hERG. [PDF]

Acta Pharmacol Sin
Ottosson NE, Frampton DJA, Pipatpolkai T, Norman C, Karlsson U, Jauregi-Miguel A, Venter M, Sridhar A, Larsson HP, Gréen H, Liin SI.   +10 more
europepmc   +1 more source

Screening the Tox21 Compound Library for Chemicals That Stimulate the Adrenergic β1 Receptor. [PDF]

Chem Res Toxicol
Adesina PA, Zhang L, Sukhawanit C, Wood S, Zhao J, Li Z, Sakamuru S, Ferguson SS, Hsieh JH, Reif DM, Huang R, Xia M.   +11 more
europepmc   +1 more source

Structure-Activity Relationship Analysis and hERG Liability Assessment of Second-Generation Antibiofilm Compounds Active Against Salmonella. [PDF]

ChemMedChem
Sorge A, Bennett AN, Gregory SE, Cole AL, Woolard KJ, Nemeth AM, Crow AH, Melander RJ, Gunn JS, Melander C.   +9 more
europepmc   +1 more source

State dependent dissociation of HERG channel inhibitors [PDF]

British Journal of Pharmacology, 2007
Background and purpose:Inhibition of HERG channels prolongs the ventricular action potential and the QT interval with the risk of torsade de pointes arrhythmias and sudden cardiac death. Many drugs induce greater inhibition of HERG channels when the cell membrane is depolarized frequently.
Manfred Auer, S Hering, E N Timin
exaly   +7 more sources

Saxitoxin Is a Gating Modifier of hERG K+ Channels [PDF]

Journal of General Physiology, 2003
Potassium (K+) channels mediate numerous electrical events in excitable cells, including cellular membrane potential repolarization. The hERG K+ channel plays an important role in myocardial repolarization, and inhibition of these K+ channels is associated with long QT syndromes that can cause fatal cardiac arrhythmias.
Paul B Bennett
exaly   +3 more sources

Astemizole Derivatives as Fluorescent Probes for hERG Potassium Channel Imaging

ACS Medicinal Chemistry Letters, 2016
The detection and imaging of hERG potassium channels in living cells can provide useful information for hERG-correlation studies. Herein, three small-molecule fluorescent probes, based on the potent hERG channel inhibitor astemizole, for the imaging of ...
Zhao Ma, Lupei Du, Minyong Li
exaly   +2 more sources

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The hERG potassium channel as a therapeutic target

Expert Opinion on Therapeutic Targets, 2007
The hERG (human ether-à-go-go-related gene) potassium channel has elicited intense scientific interest due to its counter-intuitive kinetics and its association with arrhythmia and sudden death. hERG blockade is involved in both antiarrhythmic pharmacotherapy and the pathogenesis of familial and acquired long QT syndrome (LQTS). Short QT syndrome (SQTS)
Harry J Witchel
exaly   +3 more sources

Molecular Determinants of hERG Channel Block

Molecular Pharmacology, 2006
Drug-induced block of cardiac hERG K+ channels causes acquired long QT syndrome. Here, we characterized the molecular mechanism of hERG block by two low-potency drugs (Nifekalant and bepridil) and two high-potency drugs 1-[2-(6-methyl-2pyridyl)ethyl]-4-(4-methylsulfonyl aminobenzoyl)piperidine (E-4031) and dofetilide).
Kamiya, K, Niwa, R, Mitcheson, JS, Sanguinetti, MC   +3 more
openaire   +3 more sources

hERG potassium channels and cardiac arrhythmia

Nature, 2006
hERG potassium channels are essential for normal electrical activity in the heart. Inherited mutations in the HERG gene cause long QT syndrome, a disorder that predisposes individuals to life-threatening arrhythmias. Arrhythmia can also be induced by a blockage of hERG channels by a surprisingly diverse group of drugs.
Michael C, Sanguinetti, Martin, Tristani-Firouzi   +1 more
openaire   +2 more sources