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Molecular determinants of hERG potassium channel inhibition by disopyramide

Journal of Molecular and Cellular Cardiology, 2012
The Class Ia antiarrhythmic drug disopyramide (DISO) causes QT interval prolongation that is potentially dangerous in acquired Long QT Syndrome but beneficial in short QT syndrome, through inhibition of the hERG-encoded channels responsible for rapid delayed rectifier K(+) current (I(Kr)).
El Harchi, A   +4 more
openaire   +3 more sources

In silico screening on the herg potassium channel

2011
Während des Arzneistoffentwicklungsprozesses scheitern fast 35% der Arzneistoffe wegen schlechter Absorption, Verteilung, Metabolismus, Ausscheidung und Toxizität (ADMET). Ein wichtiger Bestandteil dieses Scheiterns ist die Interaktion mit Anti-Target Proteinen wie Cytochrom P450, P-glycoprotein und dem hERG Kaliumkanal.
openaire   +1 more source

Cocaine Blocks HERG, but Not KvLQT1+minK, Potassium Channels

Molecular Pharmacology, 2001
Cocaine causes cardiac arrhythmias, sudden death, and occasionally long QT syndrome in humans. We investigated the effect of cocaine on the human K(+) channels HERG and KvLQT1+minK that encode native rapidly (I(Kr)) and slowly (I(Ks)) activating delayed rectifier K(+) channels in the heart. HERG and KvLQT1+minK channels were heterologously expressed in
S, Zhang   +7 more
openaire   +2 more sources

Mechanism of inhibition by olanzapine of cloned hERG potassium channels

Neuroscience Letters, 2015
Olanzapine is widely used in the treatment of schizophrenia and related psychoses. We investigated the effects of olanzapine on human ether-a-go-go related gene (hERG) channels stably expressed in human embryonic kidney (HEK) cells using the whole-cell patch-clamp technique.
Hong Joon, Lee   +2 more
openaire   +2 more sources

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Frontiers in Pharmacology, 2022
Kevin R DeMarco   +2 more
exaly  

HERG potassium channel regulation by the N-terminal eag domain

Cellular Signalling, 2012
Matthew C Trudeau
exaly  

hERG potassium channel gating is mediated by N- and C-terminal region interactions

Journal of General Physiology, 2011
Matthew C Trudeau
exaly  

Inhibition of the current of heterologously expressed HERG potassium channels by imipramine and amitriptyline

British Journal of Pharmacology, 1999
Elizabeth P Seward, Harry J Witchel
exaly  

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