2006-01-01, English, Article, Journal or magazine article edition: Carvedilol blocks beta(2)- more than beta(1)-adrenoceptors in human heart Molenaar, Peter; Christ, Torsten; Ravens, Ursula; ...

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Physical Description
  • journal article
Published
  • Oxford University Press, 2006-01-01
Language
  • English

Edition details

Title
  • Carvedilol blocks beta(2)- more than beta(1)-adrenoceptors in human heart
Author
  • Molenaar, Peter
  • Christ, Torsten
  • Ravens, Ursula
  • Kaumann, Alberto
Other Contributors
  • H. M. Piper
Published
  • Oxford University Press, 2006-01-01
Physical Description
  • journal article
Subjects
Summary
  • Objective: To understand the basis of the effectiveness of carvedilol in heart failure by determining its specific properties at human heart and beta(2)-adrenoceptors. Methods: The positive inotropic effects of noradrenaline (in the presence of the beta(2)-selective antagonist ICI118551) and adrenaline (in the presence of the beta(1)-selective antagonist CGP20712), mediated through beta(1)- and beta(2)-adrenoceptors, respectively, were investigated in atrial and ventricular trabeculae. The patch-clamp technique was used to investigate effects of noradrenaline and adrenaline on L-type Ca2+ current in human atrial myocytes. Results: Carvedilol was a 13-fold more potent competitive antagonist of the effects of adrenaline at 1 2-adrenoceptors (-logK(B) =​ 10.13 +/​- 0.08) than of noradrenaline at beta(1)-adrenoceptors (-logK(B) =​ 9.02 +/​- 0.07) in human right atrium. Chronic carvedilol treatment of patients with non-terminal heart failure reduced the inotropic sensitivity of atrial trabeculae to noradrenaline and adrenaline 5.6-fold and 91.2-fold, respectively, compared to beta(1)-blocker-treated patients, consistent with persistent preferential blockade of beta(2)-adrenoceptors. In terminal heart failure carvedilol treatment reduced 1.8-fold and 25.1-fold the sensitivity of right ventricular trabeculae to noradrenaline and adrenaline, respectively, but metoprolol treatment did not reduce the sensitivity to the catecholamines. Increases of current (I-Ca,I-L) produced by noradrenaline and adrenaline were not different in atrial myocytes obtained from non-terminal heart failure patients treated with metoprolol or carvedilol, consistent with dissociation of both beta-blockers from the receptors. Conclusions: Carvedilol blocks human cardiac beta(2)-adrenoceptors more than beta(1)-adrenoceptors, thereby conceivably contributing to the beneficial effects in heart failure. The persistent blockade of beta-adrenoceptors is attributed to accumulation of carvedilol in cardiac tissue. (c) 2005 European Society of Cardiology. Published by Elsevier B.V. All rights reserved.
Language
  • English
Related Resource
Identifier
  • oai:espace.library.uq.edu.au:UQ:79662

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