Identification | Back Directory | [Name]
Pilsicainide hydrochloride | [CAS]
88069-49-2 | [Synonyms]
Pilsinic Alisrythm Rizumcote Tatsupilljin PILSICAININIDE Pilsicainide hydrochoride Pilsicainide-Hydrochlordie Pilzicainide hydrochloride PILSICAINIDE HYDROCHLORIDE Pilsicainide hydrochloride USP/EP/BP PILSICAINIDE HYDROCHLORIDE HEMIHYDRATE PILSICAINIDEHYDROCHLORIDE(FORRESEARCHONLY) Pilsicainide Hydrochloride and intermediates C17H24N2O Pilsicainide hydrochloride 88069-49-2 N-(2,6-Dimethylphenyl)-2-(hexahydro-1H-pyrrolizin-7a-yl)acetamide hydrochloride n-(2,6-dimethylphenyl)-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-yl)acetamide hydrochloride | [Molecular Formula]
C17H24N2O | [MDL Number]
MFCD00864748 | [MOL File]
88069-49-2.mol | [Molecular Weight]
272.39 |
Chemical Properties | Back Directory | [Melting point ]
212-214° | [storage temp. ]
room temp | [solubility ]
Chloroform (Slightly), Water (Slightly) | [form ]
powder | [color ]
white to beige |
Safety Data | Back Directory | [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) |
Hazard Information | Back Directory | [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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