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

Names

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

[Synonym ]:
MJ-9067[AS BASE]
MJ-9067
Enkaid
Encainida [spanish]
M-9067-1
4-methoxy-N-<2-<2-(1-methyl-2-piperidinyl)ethyl>phenyl>benzamide
Encainide [french]
Encainidum
Enkade
[14C]-Encainide
Encainida
(-)-Encainide
BENZAMIDE, 4-METHOXY-N-[2-[2-(1-METHYL-2-PIPERIDINYL)ETHYL]PHENYL]-
4-methoxy-2'-[2-(1-methyl-2-piperidyl)ethyl]benzanilide

Biological Activity

[Description]:

Encainide (MJ9067) is an antiarrhythmic drug with class ⅠC activity. Encainide has the potential for life-threatening ventricular arrhythmias, symptomatic ventricular arrhythmias and supraventricular arrhythmias research[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Others >> Others

[In Vivo]

Encainide (0.3, 0.9, 2.7 mg/kg; infusion of single doses) prolongs His-Purkinje conduction time (HV interval) and intra-ventricular conduction time (QRS duration) but has no effect on sinus nodal recovery time or AV nodal conduction, or on refractoriness of atrium, AV node, or ventricular myocardium or on QT interval[1].

[References]

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

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₈N₂O₂

[ Molecular Weight ]:
352.47000

[ Exact Mass ]:
352.21500

[ PSA ]:
41.57000

[ LogP ]:
4.37530

Toxicological Information

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