Novel Potent hERG Potassium Channel Enhancers And Their In Vitro Antiarrhythmic Activity
نویسندگان
چکیده
منابع مشابه
High-affinity blockade of human ether-a-go-go-related gene human cardiac potassium channels by the novel antiarrhythmic drug BRL-32872.
Human ether-a-go-go-related gene (HERG) potassium channels are one primary target for the pharmacological treatment of cardiac arrhythmias by class III antiarrhythmic drugs. These drugs are characterized by high antiarrhythmic efficacy, but they can also initiate life-threatening "torsade de pointes" tachyarrhythmias. Recently, it has been suggested that combining potassium and calcium channel ...
متن کاملThe inhibitory effects of DC031050, a class III antiarrhythmic agent with high selectivity for hERG channels, on three neuronal potassium channels
Aim: This study was conducted to test the selectivity of a class III antiarrhythmic agent, DC031050, on cardiac hERG and neuronal potassium channels. Methods: Whole-cell voltage patch clamp was used. Results: We previously reported that DC031050, a derivative of dofetilide, exhibited more potent biological activity than its leading compound, dofetilide. Here, we show that DC031050 selectively i...
متن کاملAntiarrhythmic drug carvedilol inhibits HERG potassium channels.
OBJECTIVE 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 appeared to be superior to other...
متن کاملNatural products modulating the hERG channel: heartaches and hope† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c7np00014f
Covering: 1996-December 2016The human Ether-à-go-go Related Gene (hERG) channel is a voltage-gated potassium channel playing an essential role in the normal electrical activity in the heart. It is involved in the repolarization and termination of action potentials in excitable cardiac cells. Mutations in the hERG gene and hERG channel blockage by small molecules are associated with increased ri...
متن کاملMiRP1 Forms IKr Potassium Channels with HERG and Is Associated with Cardiac Arrhythmia
A novel potassium channel gene has been cloned, characterized, and associated with cardiac arrhythmia. The gene encodes MinK-related peptide 1 (MiRP1), a small integral membrane subunit that assembles with HERG, a pore-forming protein, to alter its function. Unlike channels formed only with HERG, mixed complexes resemble native cardiac IKr channels in their gating, unitary conductance, regulati...
متن کامل