Indecainid

Names

[ Name ]:
Indecainid

[Synonym ]:
Indecainide hydrochloride (USAN)
9-(3-((1-Methylethyl)amino)propyl)-9H-fluorene-9-carboxamide hydrochloride
9H-Fluorene-9-carboxamide,9-(3-((1-methylethyl)amino)propyl)-,monohydrochloride
Indecainide HCl
Indecainide hydrochloride
Decabid (TN)

Biological Activity

[Description]:

Indecainide hydrochloride is a potent and orally active class I local anesthetic antiarrhythmic agent[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Others >> Others

[In Vivo]

Indecainide hydrochloride (0, 3, 6, or 9 mg/kg; IV, daily for 1 month) causes 6 of 10 male rats and 1 of 10 female rats die at 9 mg/kg during the test period[2]. Indecainide hydrochloride (0, 1.5, 3, or 4.5 mg/kg; IV, daily for 1 month) causes 2 of 4 dogs die at 4.5 mg/kg; exhibits no overt signs of toxicity and no hematologic, serum chemistry or histologic changes at 1.5 or 3 mg/kg[2].

[References]

[1]. Steinberg MI, et al. Electrophysiological studies of indecainide hydrochloride, a new antiarrhythmic agent, in canine cardiac tissues. J Cardiovasc Pharmacol. 1984 Jul-Aug;6(4):614-21.

[2]. Sandusky GE Jr, et al. Toxicology of indecainide hydrochloride after intravenous administration to rats and dogs. Toxicol Lett. 1985 Aug;26(2-3):107-10.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₂₄N₂O

[ Molecular Weight ]:
308.41700

[ Exact Mass ]:
308.18900

[ PSA ]:
56.11000

[ LogP ]:
4.75720

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: LL6010000

CHEMICAL NAME :: 9H-Fluorene-9-carboxamide, 9-(3-((1-methylethyl)amino)propyl)-, monohydrochloride

CAS REGISTRY NUMBER :: 73681-12-6

LAST UPDATED :: 199406

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C20-H24-N2-O.Cl-H

MOLECULAR WEIGHT :: 344.92

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 :: 82 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Behavioral - muscle weakness

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 5,175,1985

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 10 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: TOLED5 Toxicology Letters. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1977- Volume(issue)/page/year: 26,107,1985

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 96 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Behavioral - muscle weakness

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 5,175,1985

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 25 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 5,175,1985

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >5 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: TOLED5 Toxicology Letters. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1977- Volume(issue)/page/year: 26,107,1985

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: >50 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 5,175,1985 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 270 mg/kg/30D-I

TOXIC EFFECTS :: Endocrine - changes in pituitary weight Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

REFERENCE :: TOLED5 Toxicology Letters. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1977- Volume(issue)/page/year: 26,107,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 1138 mg/kg/13W-I

TOXIC EFFECTS :: Related to Chronic Data - death

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 5,175,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 135 mg/kg/30D-I

TOXIC EFFECTS :: Cardiac - EKG changes not diagnostic of specified effects Related to Chronic Data - death

REFERENCE :: TOLED5 Toxicology Letters. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1977- Volume(issue)/page/year: 26,107,1985