pilsicainide

Modify Date: 2024-01-08 00:32:22

pilsicainide Structure
pilsicainide structure
 Common Name pilsicainide
CAS Number 88069-67-4 Molecular Weight 272.38500
Density 1.11 g/cm3 Boiling Point 416.9ºC at 760 mmHg
Molecular Formula C17H24N2O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of pilsicainide


Pilsicainide (SUN 1165 free acid) is a potent sodium channel blocker and potent class Ic antiarrhythmic agent[1][2].

 Names

Name N-(2,6-dimethylphenyl)-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-yl)acetamide
Synonym More Synonyms

 pilsicainide Biological Activity

Description Pilsicainide (SUN 1165 free acid) is a potent sodium channel blocker and potent class Ic antiarrhythmic agent[1][2].
Related Catalog
In Vitro Pilsicainide (SUN 1165 free acid; 10-200 μg/mL) decreases peak amplitude of the net inward current in a dose-dependent manner with an IC50 of 29.2 μg/mL in levo-thyroxine (T4)-treated rat atrial cells[1].
In Vivo Pilsicainide (SUN 1165 free acid; 2 mg/kg; i.v.; once) decreases the conduction velocity in T4-treated rat atrium by decreasing the Max dV/dt and net inward current[1]. Animal Model: Male Sprague-Dawley (SD) rats weighing from 200 to 220 g, with levo-thyroxine (T4) treatment[1] Dosage: 2 mg/kg Administration: Bolus injection into right external carotid vein within 2 minutes, once Result: Elongated the QT interval at 15 and 60 minutes after administration. Shortened P wave and QRS complex durations. Markedly decreased action potential amplitudes (APA) and Max dV/dt, and significantly lengthened the action potential durations.

 Chemical & Physical Properties

Density 1.11 g/cm3
Boiling Point 416.9ºC at 760 mmHg
Molecular Formula C17H24N2O
Molecular Weight 272.38500
Exact Mass 272.18900
PSA 32.34000
LogP 3.27130
Index of Refraction 1.581
Storage condition room temp

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UY7758100
CHEMICAL NAME :
1H-Pyrrolizine-7a(5H)-acetamide, tetrahydro-N-(2,6-dimethylphenyl)-, hydrochloride, hemihydrate
CAS REGISTRY NUMBER :
88069-67-4
LAST UPDATED :
199404
DATA ITEMS CITED :
7
MOLECULAR FORMULA :
C17-H24-N2-O.Cl-H.1/2H2-O
MOLECULAR WEIGHT :
317.88

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
255 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 22,769,1991
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
105 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 22,769,1991
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
18 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 22,769,1991
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
175 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 22,769,1991
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
85 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 22,769,1991
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
17 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 22,769,1991
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
53 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 22,769,1991

 Safety Information

Hazard Codes Xn
Risk Phrases 22
HS Code 2933990090

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

Pilzicainide
Pilsicainide HCl
Pilsicainida [INN-Spanish]
n-(2,6-dimethylphenyl)-8-pyrrolizidineacetamide
Pilsicainidum [INN-Latin]
Pilsicainide
Pilsicainide [INN]
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Related Compounds: More...
pilsicainide
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Pilsicainide HCl
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