Vemakalant Chemical Properties

Boiling point:

479.0±45.0 °C(Predicted)

Density 

1.14±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO

form 

Powder

pka

14.79±0.20(Predicted)

Vemakalant Usage And Synthesis

Pharmacological action

Venakaran works by blocking peak sodium currents by blocking overdrive-activated delayed rectifier currents (IKur). IKur, encoded by the Kv1.5 channel protein, is abundantly expressed in atrial myocytes, is the main current mediating atrial repolarization in humans, and is activated during atrial fibrillation. Venakalan inhibition of IKur can prolong the action potential duration of the atrium, thereby prolonging the atrial effective refractory period and slowing down atrial conduction, so as to shorten the time of atrial fibrillation and quickly achieve the effect of atrial fibrillation conversion.

Application

Venakalan is a mixed sodium/potassium channel blocker that selectively acts on atrial ion channels. It is more effective than amiodarone in the acute conversion of newly diagnosed atrial fibrillation and is used clinically to treat atrial fibrillation.

Description

Vernakalant is a potassium channel blocker that was approved in Europe in 2010 for treatment of atrial fibrillation (AF), a condition of cardiac arrhythmia in which the atria of the heart beat irregularly due to changes in cardiac ion channel function and distribution. Vernakalant has activity for cardiac Na+ and K+ channels and also for the atrial-selective Kv1.5 channel. Vernakalant (RSD1235) was characterized in animal models to assess efficacy, atrial selectivity, and reduction in side effects.

Originator

Cardiome Pharma Corp. (Canada)

Definition

ChEBI: Vernakalant is an alcohol and a member of phenols.

brand name

Brinavess

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