88069-49-2

Pilsicainide hydrochloride is a new pynolizidine lidocaine derivative with antiarrhythmic activity. It is the first pharmaceutical product introduced by Suntory and was solely developed in Japan. The compound is reported to be highly effective in the treatment of premature ventricular contraction. It has no anticholinergic or CNS activity and is not as likely as other class 1C antiarrhythmics to have restricted indications.

Suntory (Japan)

Sunrhythm

Pilsicainide hydrochloride is a pure sodium channel blocker and an open channel blocker of Na+1 channels. Pilsicainide was defined as a pure sodium channel blocker. The compound is classified as a class Ic antiarrhythmic drug, and was originally developed in Japan. Similar to Lidocaine, Pilsicainide binds to open channels, but slowly. Pilsicainide is capable of selectively blocking the late currents in the mutant Na(+) channels that show dominant abnormal burst openings such as in δKPQ mutants. The compound is used to induce Brugada syndrome (BS) in animal models.