Results 181 to 190 of about 1,218,415 (224)

Effects of donepezil on hERG potassium channels

Brain Research, 2015
Donepezil is a potent, selective inhibitor of acetylcholinesterase, which is used for the treatment of Alzheimer's disease. Whole-cell patch-clamp technique and Western blot analyses were used to study the effects of donepezil on the human ether-a-go-go-related gene (hERG) channel.
Yun Ju, Chae, Hong Joon, Lee, Ji Hyun, Jeon, In-Beom, Kim, Jin-Sung, Choi, Ki-Wug, Sung, Sang June, Hahn   +6 more
openaire   +2 more sources

HERG K+ channels: friend and foe

Trends in Pharmacological Sciences, 2001
The K+ channel encoded by the human ether-à-go-go related gene (HERG) is one of many ion channels that are crucial for normal action potential repolarization in cardiac myocytes. HERG encodes the pore-forming subunit of the rapid component of the delayed rectifier K+ channel, I(K(Vr)).
J I, Vandenberg, B D, Walker, T J, Campbell   +2 more
openaire   +2 more sources

Escitalopram block of hERG potassium channels

Naunyn-Schmiedeberg's Archives of Pharmacology, 2013
Escitalopram, a selective serotonin reuptake inhibitor, is the pharmacologically active S-enantiomer of the racemic mixture of RS-citalopram and is widely used in the treatment of depression. The effects of escitalopram and citalopram on the human ether-a-go-go-related gene (hERG) channels expressed in human embryonic kidney cells were investigated ...
Yun Ju, Chae, Ji Hyun, Jeon, Hong Joon, Lee, In-Beom, Kim, Jin-Sung, Choi, Ki-Wug, Sung, Sang June, Hahn   +6 more
openaire   +2 more sources

IKr: The hERG Channel

Journal of Molecular and Cellular Cardiology, 2001
G.-N. Tseng. I(Kr): The hERG Channel. Journal of Molecular and Cellular Cardiology (2001) 33, 835-849. The rapid delayed rectifier (I(Kr)) channel is important for cardiac action potential repolarization. Suppressing I(Kr)function, due to either genetic defects in its pore-forming subunit (hERG) or adverse drug effects, can lead to long-QT (LQT ...
openaire   +2 more sources

Pharmacophore modeling for hERG channel facilitation

Biochemical and Biophysical Research Communications, 2012
Human ether-a-go-go-related gene (hERG) channels play a critical role in cardiac action potential repolarization. The unintended block of hERG channels by compounds can prolong the cardiac action potential duration and induce arrhythmia. Several compounds not only block hERG channels but also enhance channel activation after the application of a ...
Yuko, Yamakawa, Kazuharu, Furutani, Atsushi, Inanobe, Yuko, Ohno, Yoshihisa, Kurachi   +4 more
openaire   +2 more sources

An Automated Docking Protocol for hERG Channel Blockers

Journal of Chemical Information and Modeling, 2013
A docking protocol aimed at obtaining a consistent qualitative and quantitative picture of binding for a series of hERG channel blockers is presented. To overcome the limitations experienced by standard procedures when docking blockers at hERG binding site, we designed a strategy that explicitly takes into account the conformations of the channel ...
DI MARTINO, GIOVANNI PAOLO, MASETTI, MATTEO, CECCARINI, LUISA, CAVALLI, ANDREA, RECANATINI, MAURIZIO   +4 more
openaire   +4 more sources

Open Channel Block of HERG K⁺Channels by Vesnarinone

Molecular Pharmacology, 2001
Vesnarinone, a cardiotonic agent, blocks I(Kr) and, unlike other I(Kr) blockers, produces a frequency-dependent prolongation of action potential duration (APD). To elucidate the mechanisms, we studied the effects of vesnarinone on HERG, the cloned human I(Kr) channel, heterologously expressed in Xenopus laevis oocytes.
K, Kamiya, J S, Mitcheson, K, Yasui, I, Kodama, M C, Sanguinetti   +4 more
openaire   +2 more sources

hERG Channel Inhibitors in Extracts of Coptidis Rhizoma

Planta Medica, 2011
Inhibition of the hERG channel delays repolarization and prolongs the QT interval and cardiac action potential which can lead to sudden death. Several drugs have been withdrawn from the market due to hERG channel inhibition. In the search of hERG channel inhibitors of natural origin, we established an HPLC-based profiling approach which combines HPLC ...
Schramm, A., Baburin, I., Hering, S., Hamburger, M.   +3 more
openaire   +5 more sources

HERG channel trafficking.

Novartis Foundation symposium, 2005
Mutations in the cardiac potassium channel hERG/IKr cause inherited long QT syndrome with increased susceptibility to ventricular arrhythmias. Several mutations in hERG produce trafficking-deficient channels that are retained in the endoplasmic reticulum (ER). Surface expression of certain mutations (i.e. hERG G601S) can be restored by specific channel
Eckhard, Ficker, Adrienne, Dennis, Yuri, Kuryshev, Barbara A, Wible, Arthur M, Brown   +4 more
openaire   +1 more source

The hERG potassium channel and hERG screening for drug-induced torsades de pointes

Pharmacology & Therapeutics, 2008
Drug-induced torsades de pointes (TdP) arrhythmia is a major safety concern in the process of drug design and development. The incidence of TdP tends to be low, so early pre-clinical screens rely on surrogate markers of TdP to highlight potential problems with new drugs.
Hancox, JC, McPate, MJW, El Harchi, A, Zhang, YH   +3 more
openaire   +3 more sources