Document Detail


Carvedilol blockade of alpha1- and beta-adrenoceptor induced inotropic responses in rats with congestive heart failure.
MedLine Citation:
PMID:  15916756     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Carvedilol is a combined alpha(1)- and beta-adrenoceptor antagonist. We investigated the ability of carvedilol to antagonize functional effects mediated through myocardial alpha(1)-adrenoceptors in failing vs. non-failing (sham-operated) control hearts and compared such antagonisms to those of myocardial beta-adrenoceptors. Congestive heart failure was induced in Wistar rats by coronary artery ligation. Papillary muscles experiments were performed. Carvedilol antagonized inotropic effects mediated through myocardial alpha(1)-adrenoceptors with similar potencies in failing (pK(i)=7.7 (95%, CI; 7.4-8.0)) and sham-operated hearts (pK(i)=7.9 (95%, CI; 7.6-8.1)). The potency for the alpha(1)-adrenoceptors was 10-30-fold lower than that for the beta-adrenoceptors. In failing hearts, the alpha(1)-adrenoceptor mediated response was similar in size to the attenuated beta-adrenoceptor mediated inotropic response. The beta-adrenoceptor mediated lusitropic effects were not, however, attenuated in failing compared to sham-operated hearts. A low degree of alpha(1)-adrenoceptor blockade in the myocardium may contribute to the beneficial effects of carvedilol in heart failure.
Authors:
Eirik Qvigstad; Ivar Sjaastad; Janny Bøkenes; Iwona Schiander; Line Solberg; Ole M Sejersted; Jan-Bjørn Osnes; Tor Skomedal
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Publication Detail:
Type:  Comparative Study; In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  European journal of pharmacology     Volume:  516     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  2005 May 
Date Detail:
Created Date:  2005-06-06     Completed Date:  2005-08-29     Revised Date:  2013-05-28    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  51-9     Citation Subset:  IM    
Affiliation:
Department of Pharmacology, University of Oslo, P.O. Box 1057 Blindern, N-0316 Oslo, Norway. eirik.qvigstad@labmed.uio.no
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MeSH Terms
Descriptor/Qualifier:
Adrenergic alpha-Antagonists / pharmacology
Adrenergic beta-Agonists / pharmacology
Adrenergic beta-Antagonists / pharmacology
Animals
Carbazoles / pharmacology*
Dose-Response Relationship, Drug
Heart Failure / etiology,  physiopathology*
Isoproterenol / pharmacology
Male
Myocardial Contraction / drug effects*
Myocardial Infarction / complications
Norepinephrine / pharmacology
Papillary Muscles / drug effects,  physiopathology
Phenylephrine / pharmacology
Propanolamines / pharmacology*
Rats
Rats, Wistar
Receptors, Adrenergic, alpha-1 / physiology*
Receptors, Adrenergic, beta / physiology*
Vasoconstrictor Agents / pharmacology
Vasodilator Agents / pharmacology
Chemical
Reg. No./Substance:
0/Adrenergic alpha-Antagonists; 0/Adrenergic beta-Agonists; 0/Adrenergic beta-Antagonists; 0/Carbazoles; 0/Propanolamines; 0/Receptors, Adrenergic, alpha-1; 0/Receptors, Adrenergic, beta; 0/Vasoconstrictor Agents; 0/Vasodilator Agents; 0K47UL67F2/carvedilol; 51-41-2/Norepinephrine; 59-42-7/Phenylephrine; 7683-59-2/Isoproterenol

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


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