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Indecainid

Indecainid用途

盐酸依地卡因是一种有效的口服I类局部麻醉药抗心律失常剂[1]。

Indecainid名称

[ CAS 号 ]:
73681-12-6

[ 英文名 ]:
Indecainid

[英文别名 ]:

Indecainide hydrochloride (USAN)
Indecainide HCl
Indecainide hydrochloride
Decabid (TN)

Indecainid生物活性

[ 描述 ]:

盐酸依地卡因是一种有效的口服I类局部麻醉药抗心律失常剂[1]。

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> 其他 >> 其他

[体内研究]

盐酸依地卡因(0、3、6或9 mg/kg；IV,每天1个月)导致10只雄性大鼠中有6只在试验期间死亡,10只雌性大鼠中的1只在9 mg/kg时死亡[2]。盐酸依地卡因(0、1.5、3或4.5毫克/千克；静脉注射,每天1个月)导致4只狗中有2只在4.5 mg/千克时死亡；在1.5 mg/kg或3 mg/kg时,没有明显的毒性迹象,也没有血液学、血清化学或组织学变化[2]。

[参考文献]

[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.

Indecainid物理化学性质

[ 分子式 ]:
C₂₀H₂₄N₂O

[ 分子量 ]:
308.41700

[ 精确质量 ]:
308.18900

[ PSA ]:
56.11000

[ LogP ]:
4.75720

Indecainid毒性和生态

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