| Mechanism of cardiovascular action of trapidil. | |
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MedLine Citation:
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PMID: 6254546 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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K Satoh; S Yamashita; M Endoh; N Taira |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Arzneimittel-Forschung Volume: 30 ISSN: 0004-4172 ISO Abbreviation: Arzneimittelforschung Publication Date: 1980 |
Date Detail:
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Created Date: 1981-01-26 Completed Date: 1981-01-26 Revised Date: 2007-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0372660 Medline TA: Arzneimittelforschung Country: GERMANY, WEST |
Other Details:
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Languages: eng Pagination: 1264-8 Citation Subset: IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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3',5'-Cyclic-AMP Phosphodiesterases
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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:
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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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