(±)-4-甲氧基-N-[2-[2-(1-甲基-2-哌啶基)乙基]苯基]苯甲酰胺

用途

Encainide(MJ9067)是一种具有ⅠC活动。Encainide有可能用于威胁生命的室性心律失常、症状性室性心律失常和室上性心律失常的研究[1]。

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名称

[ CAS 号 ]:
66778-36-7

[ 中文名 ]:
(±)-4-甲氧基-N-[2-[2-(1-甲基-2-哌啶基)乙基]苯基]苯甲酰胺

[ 英文名 ]:
BENZAMIDE, 4-METHOXY-N-[2-[2-(1-METHYL-2-PIPERIDINYL)ETHYL]PHENYL]-

[中文别名 ]:

[英文别名 ]:

MJ-9067[AS BASE]
MJ-9067
Enkaid
Encainida [spanish]
M-9067-1
Encainide [french]
Encainidum
Enkade
[14C]-Encainide
Encainida

生物活性

[ 描述 ]:

Encainide(MJ9067)是一种具有ⅠC活动。Encainide有可能用于威胁生命的室性心律失常、症状性室性心律失常和室上性心律失常的研究[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]

恩卡肽(0.3,0.9,2.7 mg/kg；单剂量输注)可延长其浦肯野传导时间(HV间期)和心室内传导时间(QRS持续时间),但对窦房结恢复时间或房室结传导,或心房、房室结或心室心肌的难治性或QT间期无影响[1]。

[参考文献]

[1]. R N Brogden, et al. Encainide. A review of its pharmacological properties and therapeutic efficacy. Drugs. 1987 Nov;34(5):519-38.

物理化学性质

[ 分子式 ]:
C₂₂H₂₈N₂O₂

[ 分子量 ]:
352.47000

[ 精确质量 ]:
352.21500

[ PSA ]:
41.57000

[ LogP ]:
4.37530

毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CV5521000

CHEMICAL NAME :: Benzamide, 4-methoxy-N-(2-(2-(1-methyl-2-piperidinyl)ethyl)pheny l)-, (+-)-

CAS REGISTRY NUMBER :: 66778-36-7

BEILSTEIN REFERENCE NO. :: 0497572

LAST UPDATED :: 199612

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C22-H28-N2-O2

MOLECULAR WEIGHT :: 352.52

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - infant

DOSE/DURATION :: 3289 ug/kg

TOXIC EFFECTS :: Cardiac - arrhythmias (including changes in conduction) Cardiac - change in rate

REFERENCE :: AEMED3 Annals of Emergency Medicine. (American College of Emergency Physicians, 1125 Executive Circle, Irving, TX 75038) Volume(issue)/page/year: 21,998,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 43 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Cardiac - pulse rate increase, without fall in BP Vascular - BP lowering not characterized in autonomic section

REFERENCE :: AJCDAG American Journal of Cardiology. (Technical Pub. Co., 875 Third Ave., New York, NY 10022) V.1- 1958- Volume(issue)/page/year: 57,878,1986

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 3214 mg/kg/19H

TOXIC EFFECTS :: Cardiac - cardiomyopathy including infarction Cardiac - arrhythmias (including changes in conduction)

REFERENCE :: AHJOA2 American Heart Journal. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1925- Volume(issue)/page/year: 102,857,1981

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 2400 ug/kg/17H

TOXIC EFFECTS :: Cardiac - cardiomyopathy including infarction Cardiac - arrhythmias (including changes in conduction)

REFERENCE :: AHJOA2 American Heart Journal. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1925- Volume(issue)/page/year: 102,857,1981

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 1500 ug/kg

TOXIC EFFECTS :: Cardiac - arrhythmias (including changes in conduction)

REFERENCE :: AHJOA2 American Heart Journal. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1925- Volume(issue)/page/year: 102,857,1981

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 38100 ug/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 281,277,1986