Azimilide dihydrochloride may be used in the electrophysiology experiments with human ether-a-go-go-related gene 1a (HERG1a) subunit.[1]
Biochem/physiol Actions
Azimilide is a Class III antiarrhythmic; blocker of the delayed rectifier cardiac potassium channels; inhibits KV7.1 and KV11.1 potassium channels.
Azimilide is an inhibitor of human ether-a-go-go-related gene (HERG) channel. It displays a decrease in inhibitory effect in acidic pH conditions.[2]
Azimilide is an investigational class III anti-arrhythmic drug that blocks fast and slow components of the delayed rectifier cardiac potassium channels. It inhibits KV7.1 and KV11.1 potassium channels. Azimilide′s block of K+ currents is relatively selective for IKr over IKs: It potently blocks the rapidly activating component of the delayed rectifier, IKr (IC50 0.4 mM), and inhibits IKs (IC50 3 mM) with nearly 10-fold less potency. At 10 mM, it does not block the inward rectifier K+ current. It blocks (10 mM) the L-type Ca2+ current (ICa) in a use-dependent manner.
Features and Benefits
This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Acidosis is one of the important deleterious factors during myocardial ischaemia and reperfusion. The ether-a-go-go-related gene, HERG, is a primary target for blockade by many drugs including dofetilide, quinidine and azimilide. While most drugs lose their efficacy against arrhythmias associated
The American journal of cardiology, 102(6A), 12H-19H (2008-10-22)
Pharmacologic antiarrhythmic therapy is the most commonly used treatment in most patients with atrial fibrillation (AF), but currently available agents are limited by risks that may offset the benefits of sinus rhythm. The development of antiarrhythmic agents with the potential
Journal of pharmacological sciences, 114(1), 111-114 (2010-08-17)
We examined the effect of azimilide, a class III antiarrhythmic drug, on Na(+)/Ca(2+) exchange current (I(NCX)) in guinea-pig cardiac single ventricular cells. External application of azimilide suppressed bi-directional I(NCX) in a concentration-dependent manner. IC(50) values for outward and inward I(NCX)
Current cardiology reports, 9(5), 381-386 (2007-09-20)
Implantable cardioverter defibrillators (ICDs) are now the mainstay of therapy in patients with sustained ventricular tachycardia (VT), ventricular fibrillation, resuscitated sudden cardiac death, or certain high-risk markers for these arrhythmic events. Although ICDs in such patients can be life-saving, they
European heart journal, 27(24), 3027-3032 (2006-10-20)
The purpose of this study was to assess the incidence, features, and clinical sequelae of 'electrical storm' (ES). This study is a prospectively designed secondary analysis of SHIELD; a randomized trial of azimilide for suppression of ventricular tachycardia/fibrillation (VT/VF) leading
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