Results 31 to 40 of about 1,529,868 (197)

Phα1β interaction with the Kv11.1 potassium channel in HEK293 cells transfected with the human ERG channel [PDF]

Journal of Venomous Animals and Toxins including Tropical Diseases
Background: This study examines the impact of Phα1β, a spider peptide derived from the venom of Phoneutria nigriventer, on the Kv11.1 potassium channel in HEK293 cells transfected with the human ERG potassium channel.
João B. Calixto, Adara Aurea dos Santos, Juliano Ferreira, Alessandra Hubner Souza, Célio José de Castro Junior, Marcus Vinicius Gomez   +5 more
doaj   +1 more source

Mechanisms of hERG Potassium Channel Enhancers [PDF]

Biophysical Journal, 2011
Mutations in the human Ether-a-go-go related gene (hERG) potassium channel and hERG channel blockers offer tools for studying structural, biophysical and functional properties of the channel. However, the current understanding of how the hERG channel opens and closes is still incomplete. Here, we used alternative chemical tools, hERG channel enhancers,
Lin, Chia-Wei, Cao, Xueying, Penland, Robert, Urban, Laszlo, Erdemli, Gul   +4 more
openaire   +1 more source

Chronic Administration of COVID-19 Drugs Fluvoxamine and Lopinavir Shortens Action Potential Duration by Inhibiting the Human Ether‐à‐go‐go–Related Gene and Cav1.2

Frontiers in Pharmacology, 2022
Background: Old drugs for new indications in the novel coronavirus disease of 2019 (COVID-19) pandemic have raised concerns regarding cardiotoxicity, especially the development of drug-induced QT prolongation.
Zequn Zheng, Zequn Zheng, Zequn Zheng, Dihui Cai, Dihui Cai, Yin Fu, Yin Fu, Ying Wang, Yongfei Song, Yongfei Song, Jiangfang Lian, Jiangfang Lian   +11 more
doaj   +1 more source

Alprenolol Inhibits Herg Potassium Channels [PDF]

Biophysical Journal, 2010
The action of alprenolol, a non-selective beta blocker as well as 5-HT receptor antagonist, on the cloned cardiac human ether-a-go-go-related gene (HERG) channels was investigated using the whole-cell patch-clamp technique. Alprenolol reduced HERG whole-cell currents in a reversible concentration-dependent manner, with an IC50 value and a Hill ...
Lee, Seung Ho, Lee, Hyang Mi, Choi, Bok Hee   +2 more
openaire   +1 more source

Сardioprotective agents with biaromatic structure. Part 5. Potassium Kv1.5-channels blockers

Фармакокинетика и Фармакодинамика, 2023
The Kv1.5 potassium channel provides an ultra-rapid delayed rectifier potassium current, IKur, that acts selectively in human atrial cells. This makes selective Kv1.5 blockade a promising approach to control atrial arrhythmias without the adverse ...
G. V. Mokrov
doaj   +1 more source

Increased vulnerability of human ventricle to re-entrant excitation in hERG-linked variant 1 short QT syndrome [PDF]

, 2011
The short QT syndrome (SQTS) is a genetically heterogeneous condition characterized by abbreviated QT intervals and an increased susceptibility to arrhythmia and sudden death.
Hancox Jules C., McPate, Mark J., Mark J McPate, Hancox, Jules C., Witchel, HJ, Witchel Harry J., Witchel, Harry J., Ismail Adeniran, Zhang, H., Hancox, JC, McPate, MJW, Henggui Zhang (74233), Ismail Adeniran (192479), Adeniran, I., Adeniran, Ismail, Zhang Henggui, Adeniran Ismail, Zhang, Henggui, Henggui Zhang, Jules C Hancox, Harry Witchel (4462174), Jules C Hancox (16149998), McPate Mark J., Mark J McPate (16150001), Harry J Witchel   +24 more
core   +2 more sources

hERG Blockade Prediction by Combining Site Identification by Ligand Competitive Saturation and Physicochemical Properties

Chemistry, 2022
The human ether-a-go-go-related gene (hERG) potassium channel is a well-known contributor to drug-induced cardiotoxicity and therefore is an extremely important target when performing safety assessments of drug candidates.
Himanshu Goel, Wenbo Yu, Alexander D. MacKerell   +2 more
doaj   +1 more source

Electrocardiographic Biomarkers for Detection of Drug-Induced Late Sodium Current Block. [PDF]

PLoS ONE, 2016
Drugs that prolong the heart rate corrected QT interval (QTc) on the electrocardiogram (ECG) by blocking the hERG potassium channel and also block inward currents (late sodium or L-type calcium) are not associated with torsade de pointes (e.g. ranolazine
Jose Vicente, Lars Johannesen, Meisam Hosseini, Jay W Mason, Philip T Sager, Esther Pueyo, David G Strauss   +6 more
doaj   +1 more source

Antiarrhythmic drug carvedilol inhibits HERG potassium channels [PDF]

Cardiovascular Research, 2001
The aryloxypropanolamine carvedilol is a multiple action cardiovascular drug with blocking effects on alpha-receptors, beta-receptors, Ca(2+)-channels, Na(+)-channels and various native cardiac K(+) channels, thereby prolonging the cardiac action potential. In a number of clinical trials with patients suffering from congestive heart failure, carvedilol
C A, Karle, V A, Kreye, D, Thomas, K, Röckl, S, Kathöfer, W, Zhang, J, Kiehn   +6 more
openaire   +2 more sources

Effects of cariprazine on hERG 1A and hERG 1A/3.1 potassium channels

European Journal of Pharmacology, 2019
Cariprazine is a novel atypical antipsychotic drug that is widely used for the treatment of schizophrenia and bipolar mania/mixed disorder. We used the whole-cell patch-clamp technique to investigate the effects of cariprazine on hERG channels that are stably expressed in HEK cells. Cariprazine inhibited the hERG 1A and hERG 1A/3.1 tail currents at -50
Hong Joon, Lee, Bok Hee, Choi, Jin-Sung, Choi, Sang June, Hahn   +3 more
openaire   +2 more sources