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]。
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Indecainid名称

[ CAS 号 ]:
73681-12-6

[ 英文名 ]:
Indecainid

[英文别名 ]:

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
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