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    
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.
Eirik Qvigstad; Ivar Sjaastad; Janny Bøkenes; Iwona Schiander; Line Solberg; Ole M Sejersted; Jan-Bjørn Osnes; Tor Skomedal
Related Documents :
234266 - Long-term beta blockade: possible protection from myocardial infarction.
15516856 - Biologic rationale for the use of beta-blockers in the treatment of heart failure.
9060806 - Iodine-123 metaiodobenzylguanidine myocardial scintigraphy for prediction of response t...
22517646 - Remote ischemic preconditioning immediately before percutaneous coronary intervention d...
14992906 - Neutrophil depletion reduces myocardial reperfusion morbidity.
7897826 - Coronary fistulous communications with left ventricular chamber and giant mural thrombu...
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    
Department of Pharmacology, University of Oslo, P.O. Box 1057 Blindern, N-0316 Oslo, Norway.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Adrenergic alpha-Antagonists / pharmacology
Adrenergic beta-Agonists / pharmacology
Adrenergic beta-Antagonists / pharmacology
Carbazoles / pharmacology*
Dose-Response Relationship, Drug
Heart Failure / etiology,  physiopathology*
Isoproterenol / pharmacology
Myocardial Contraction / drug effects*
Myocardial Infarction / complications
Norepinephrine / pharmacology
Papillary Muscles / drug effects,  physiopathology
Phenylephrine / pharmacology
Propanolamines / pharmacology*
Rats, Wistar
Receptors, Adrenergic, alpha-1 / physiology*
Receptors, Adrenergic, beta / physiology*
Vasoconstrictor Agents / pharmacology
Vasodilator Agents / pharmacology
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

Previous Document:  A computer simulation of in vivo tumour growth and response to radiotherapy: new algorithms and para...
Next Document:  Effects of a 5-HT2A receptor antagonist, sarpogrelate on thermal or inflammatory pain.