Results 161 to 170 of about 1,529,868 (197)

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
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Curcumin inhibits hERG potassium channels in vitro

Toxicology Letters, 2012
Curcumin is reported to exert antioxidant, anti-inflammatory, antiviral, antibacterial, antifungal, and anti-tumor activities. The human ether-a-go-go related gene (hERG) encodes the rapid component of the delayed rectifier K⁺ currents. Inhibition of hERG K⁺ channels leads to cardiac repolarization prolongation, which contributes to either the anti ...
Chao-Wei, Hu, Yue, Sheng, Qin, Zhang, Hui-Bin, Liu, Xin, Xie, Wen-Chao, Ma, Rong, Huo, De-Li, Dong   +7 more
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The Interactions Between hERG Potassium Channel and Blockers

Current Topics in Medicinal Chemistry, 2009
The human ether-a-go-go related gene (hERG) potassium channel is critical to the QT interval in the human heart measured by the electrocardiogram (ECG). The blockade of hERG would induce undesired lethal arrhythmia, named torsades de pointes (TdP), a rare but life-threatening symptom.
Lupei, Du, Minyong, Li, Qidong, You
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Aconitine blocks HERG and Kv1.5 potassium channels

Journal of Ethnopharmacology, 2010
Aconitum has been widely used to treat various diseases in China for a long time. However, improper use of this drug results in severe intoxication. Aconitine (ACO), a diterpenoid alkaloid from aconitum, mainly contributes to cardio-toxic effects of aconitum and has also been commonly known to induce arrhythmias in animal models.
Yifu, Li, Danna, Tu, Hua, Xiao, Yimei, Du, Anruo, Zou, Yuhua, Liao, Shaohong, Dong   +6 more
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Inhibition of the HERG potassium channel by the tricyclic antidepressant doxepin

Biochemical Pharmacology, 2007
HERG (human ether-à-go-go-related gene) encodes channels responsible for the cardiac rapid delayed rectifier potassium current, I(Kr). This study investigated the effects on HERG channels of doxepin, a tricyclic antidepressant linked to QT interval prolongation and cardiac arrhythmia.
Andrew F. James, D J Leishman
exaly   +3 more sources

The Phenothiazine Drugs Inhibit hERG Potassium Channels

Drug and Chemical Toxicology, 2005
Cardiovascular adverse effects from phenothiazine drugs are common. The most serious consequences of treatment, arrhythmias and sudden death, are probably rare and most likely to be caused primarily by blockade of cardiac potassium channels such as the human ether-a-go-go-related gene (hERG) channel, which plays a central role in arrhythmogenesis. This
Ki-Suk, Kim, Eun-Joo, Kim
openaire   +2 more sources

Predictive models for hERG potassium channel blockers

Bioorganic & Medicinal Chemistry Letters, 2005
We report here a general method for the prediction of hERG potassium channel blockers using computational models generated from correlation analyses of a large dataset and pharmacophore-based GRIND descriptors. These 3D-QSAR models are compared favorably with other traditional and chemometric based HQSAR methods.
CIANCHETTA, GIOVANNI, Li Y., Kang J., Rampe D., FRAVOLINI, Arnaldo, CRUCIANI, Gabriele, Vaz R. J.   +6 more
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Prediction of hERG potassium channel affinity by the CODESSA approach

Bioorganic & Medicinal Chemistry, 2006
The problem of predicting torsadogenic cardiotoxicity of drugs is afforded in this work. QSAR studies on a series of molecules, acting as hERG K+ channel blockers, were carried out for this purpose by using the CODESSA program. Molecules belonging to the analyzed dataset are characterized by different therapeutic targets and by high molecular diversity.
Coi A, Massarelli I, Murgia L, Saraceno M, CALDERONE, VINCENZO, BIANUCCI, ANNA MARIA PAOLA   +5 more
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How to Fluorescently Label the Potassium Channel: A Case in hERG

Current Medicinal Chemistry, 2020
hERG (Human ether-a-go-go-related gene) potassium channel, which plays an essential role in cardiac action potential repolarization, is responsible for inherited and druginduced long QT syndrome. Recently, the Cryo-EM structure capturing the open conformation of hERG channel was determined, thus pushing the study on hERG channel at 3.8 Å resolution ...
Xiaomeng, Zhang, Beilei, Wang, Zhenzhen, Liu, Yubin, Zhou, Lupei, Du   +4 more
openaire   +2 more sources

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