pilsicainide

Names

[ Name ]:
pilsicainide

[Synonym ]:
Pilzicainide
Pilsicainide HCl
Pilsicainida [INN-Spanish]
n-(2,6-dimethylphenyl)-8-pyrrolizidineacetamide
Pilsicainidum [INN-Latin]
Pilsicainide
Pilsicainide [INN]

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel

Research Areas >> Cardiovascular Disease

[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

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

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%