Document Detail


Antiarrhythmic and cardiovascular profiles of the fused indole compound (3aR,12R,12aR,12bS)-12-amino-2,3,3a,4,11,12,12a,12b-octahydro-10-hydrox yisoquino [2,1,8-lma]carbazol-5(1H)-one hydrochloride 1.5 hydrate.
MedLine Citation:
PMID:  1810258     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Antiarrhythmic and cardiovascular profiles of a fused indole compound, (3aR,12R,12aR,12bS)-12-amino-2,3,3a,4,11,12,12a,12b -octahydro- 10-hydroxyisoquino [2,1,8-lma]carbazol-5(1H)-one hydrochloride 1.5 hydrate (RS-2135, CAS 133775-36-7), were investigated in anesthetized dogs. Class I antiarrhythmic agents such as disopyramide, lidocaine, mexiletine and flecainide were used as reference compounds. RS-2135 exerted more potent antiarrhythmic activity than reference compounds against ouabain-induced arrhythmias in dogs. The onset of action was slow, but the duration of action was longer than with the other compounds tested. The agent suppressed the conduction in the atrium, A-V node and ventricle more markedly than the reference compounds. RS-2135, however, did not change blood pressure and heart rate at a dose 5 times the dose for antiarrhythmic activity and decreased cardiac contractility to a lesser extent than the reference compounds.
Authors:
R Yorikane; H Mizuno; Y Itoh; H Koike; S Miyake; H Shiga; S Kumakura; M Fukami; Y Shimoji; T Hashimoto
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Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  Arzneimittel-Forschung     Volume:  41     ISSN:  0004-4172     ISO Abbreviation:  Arzneimittelforschung     Publication Date:  1991 Nov 
Date Detail:
Created Date:  1992-05-26     Completed Date:  1992-05-26     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  0372660     Medline TA:  Arzneimittelforschung     Country:  GERMANY    
Other Details:
Languages:  eng     Pagination:  1130-6     Citation Subset:  IM    
Affiliation:
Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
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MeSH Terms
Descriptor/Qualifier:
Animals
Anti-Arrhythmia Agents / pharmacology*
Arrhythmias, Cardiac / chemically induced,  prevention & control
Carbazoles / pharmacology*
Chloroform
Disopyramide / pharmacology
Dogs
Female
Flecainide / pharmacology
Heart / drug effects
Heart Conduction System / drug effects
Hemodynamics / drug effects*
Isoquinolines / pharmacology*
Lidocaine / pharmacology
Male
Mexiletine / pharmacology
Mice
Mice, Inbred ICR
Myocardial Contraction / drug effects
Ouabain
Chemical
Reg. No./Substance:
0/Anti-Arrhythmia Agents; 0/Carbazoles; 0/Isoquinolines; 133775-36-7/RS 2135; 137-58-6/Lidocaine; 31828-71-4/Mexiletine; 3737-09-5/Disopyramide; 54143-55-4/Flecainide; 630-60-4/Ouabain; 67-66-3/Chloroform

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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