Pilsicainide hydrochloride Chemical Properties

Melting point:

212-214°

storage temp. 

room temp

solubility 

Chloroform (Slightly), Water (Slightly)

form 

powder

color 

white to beige

Safety Information

RIDADR 

UN 2811 6.1 / PGIII

WGK Germany 

3

HS Code 

2933.99.7000

Toxicity

LD50 in mice (mg/kg): 410 s.c. (Miyano, 1985)

Pilsicainide hydrochloride Usage And Synthesis

Description

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.

Originator

Suntory (Japan)

Uses

Pilsicainide hydrochloride has been used as a sodium channel blocker:

• to study its effects on electrophysiological parameters in guinea pig pulmonary vein preparation
• to study its effects on Ca²⁺?release and arrhythmic events in Andersen-Tawil syndrome induced pluripotent stem cells (ATS-iPSC)-derived cardiomyocytes
• to study its electrophysiological effects on the guinea pig atrium

brand name

Sunrhythm

Biochem/physiol Actions

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.

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