Document Detail


Mechanism of cardiovascular action of trapidil.
MedLine Citation:
PMID:  6254546     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
In anaesthetized, open-chest dogs N,N-diethyl-5-methyl[1,2,4]triazolo[1,5-alpha]pyrimidine-7-amine (trapidil) in doses of 0.3--3 mg/kg i.v. produced increases in coronary sinus outflow and heart rate and decreases in systemic blood pressure and coronary resistance in a dose-dependent manner. Trapidil produced an increase in myocardial oxygen consumption but virtually no change in coronary arteriovenous oxygen difference. At 1.8 mg/kg i.v. of the drug coronary resistance fell to half of the pre-drug value and coronary sinus outflow almost doubled, and so did myocardial oxygen consumption. In isolated, blood-perfused dog heart preparations, trapidil produced coronary vasodilator and positive inotropic and chronotropic effects. Theophylline produced similar effects. Trapidil was a more positive inotropic than positive chronotropic agent, and so was theophylline but to a lesser degree than trapidil. In producing vasodilator and positive inotropic effects trapidil was about 3 times more effective than theophylline. Trapidil and theophylline inhibited the cyclic AMP phosphodiesterase (PDE) activity in crude extracts prepared from the dog ventricular muscle. In this respect trapidil was nearly 3 times more potent than theophylline. It is suggested that PDE inhibition would be a fundamental mechanism of action of trapidil.
Authors:
K Satoh; S Yamashita; M Endoh; N Taira
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Arzneimittel-Forschung     Volume:  30     ISSN:  0004-4172     ISO Abbreviation:  Arzneimittelforschung     Publication Date:  1980  
Date Detail:
Created Date:  1981-01-26     Completed Date:  1981-01-26     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  0372660     Medline TA:  Arzneimittelforschung     Country:  GERMANY, WEST    
Other Details:
Languages:  eng     Pagination:  1264-8     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
3',5'-Cyclic-AMP Phosphodiesterases / antagonists & inhibitors
Animals
Dogs
Heart / drug effects
Heart Conduction System / drug effects
Hemodynamics / drug effects*
Myocardium / enzymology
Oxygen Consumption / drug effects
Papillary Muscles / drug effects
Pyrimidines / pharmacology*
Sinoatrial Node / drug effects
Theophylline / pharmacology
Trapidil / pharmacology*
Chemical
Reg. No./Substance:
0/Pyrimidines; 15421-84-8/Trapidil; 58-55-9/Theophylline; EC 3.1.4.17/3',5'-Cyclic-AMP Phosphodiesterases

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


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