| Adrenoceptor-blocking activity and cardiohemodynamic effects of carvedilol in animals. | |
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MedLine Citation:
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PMID: 1696657 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The beta-blocking activities of a new beta-adrenoceptor blocking drug, carvedilol, evaluated in isolated atria and trachea of the guinea pig were 2.0 (beta 1) and 3.2 times (beta 2), respectively, as potent as those of propranolol. Carvedilol exhibited the alpha-blocking activities in the aorta of guinea pigs and rats. Carvedilol was 2 and 50 times less potent in guinea pigs and rats, respectively, than prazosin as an alpha-blocker. Thus, the alpha-blocking activities were twice as potent as the beta-blocking activity in the rat and one-fifth that of the beta-blocking activity in the guinea pig. In anesthetized open-chest dogs, the beta-blocking activity of carvedilol was 1.5 times more potent than that of propranolol and had 3.8 times the alpha-blocking activity. Thus, carvedilol is a nonselective beta-blocking drug with a potent alpha-blocking activity. Carvedilol and propranolol showed dose-dependent and significant decreases in the blood pressure, total cardiac output, left ventricular pressure, dp/dt, heart rate, coronary flow, and oxygen consumption in anesthetized open-chest dogs. Carvedilol decreased the total peripheral resistance significantly (the decrease was not proportional to the decreases in the blood pressure at high doses), while propranolol increased it significantly and dose-dependently. These results indicate the importance of alpha-adrenoceptor blocking activity in the decrease in blood pressure produced by carvedilol. |
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Authors:
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T Kawada; T Ishibashi; M Nakazawa; S Satoh; S Imai |
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Publication Detail:
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Type: In Vitro; Journal Article |
Journal Detail:
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Title: Journal of cardiovascular pharmacology Volume: 16 ISSN: 0160-2446 ISO Abbreviation: J. Cardiovasc. Pharmacol. Publication Date: 1990 Jul |
Date Detail:
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Created Date: 1990-09-18 Completed Date: 1990-09-18 Revised Date: 2007-11-15 |
Medline Journal Info:
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Nlm Unique ID: 7902492 Medline TA: J Cardiovasc Pharmacol Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 147-53 Citation Subset: IM |
Affiliation:
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Department of Pharmacology, Niigata University School of Medicine, Japan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Adrenergic alpha-Antagonists Adrenergic beta-Antagonists / pharmacology* Animals Aorta, Thoracic / drug effects Carbazoles / pharmacology* Coronary Circulation / drug effects Dogs Female Guinea Pigs Heart / drug effects* Heart Rate / drug effects Hemodynamics / drug effects* Male Muscle Contraction / drug effects Muscle, Smooth / drug effects Muscle, Smooth, Vascular / drug effects Oxygen Consumption / drug effects Propanolamines / pharmacology* Propranolol / pharmacology Rats Trachea / drug effects |
| Chemical | |
Reg. No./Substance:
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0/Adrenergic alpha-Antagonists; 0/Adrenergic beta-Antagonists; 0/Carbazoles; 0/Propanolamines; 525-66-6/Propranolol; 72956-09-3/carvedilol |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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