Nebivolol, carvedilol and metoprolol do not influence cardiac Ca(2+) sensitivity

A Bundkirchen, K Brixius, B Bölck, U Mehlhorn, W Bloch, R H Schwinger

Publication: Contribution to journalJournal articlesResearchpeer-review

Abstract

It has been argued that some beta-adrenoceptor antagonists may directly influence myofibrillar cross-bridge interaction in cardiac skinned fiber preparations of animal models. The present study investigates the effects of nebivolol, metoprolol and carvedilol on tension development of Triton X-100 skinned fibers obtained from human failing myocardium as well as on force of contraction and intracellular Ca(2+) transient in isolated trabeculae. In skinned fiber preparations, none of the beta-adrenoceptor antagonists (10 microM) influenced Ca(2+) sensitivity of tension development or maximal Ca(2+) activated tension (DT(max)): control: EC(50) for Ca(2+): 1.28+/-0.05 microM, DT(max): 14.09+/-0.59 mN/mm(2); nebivolol: 1.36+/-0.1 microM, 14.14+/-0.95 mN/mm(2); carvedilol: 1.32+/-0.11 microM, 13.83+/-0.90 mN/mm(2); metoprolol: 1.34+/-0.14 microM, 13.72+/-0.36 mN/mm(2). Simultaneous measurement of force and Ca(2+) transient in the presence of the beta-adrenoceptor antagonists (3 microM) showed that the decrease in force of contraction was paralleled by a similar decrease in the intracellular Ca(2+) transient. In conclusion, none of the investigated beta-adrenoceptor antagonists influenced Ca(2+) sensitivity of myofibrillar tension development in human failing myocardium.

Original languageEnglish
JournalEuropean journal of pharmacology
Volume422
Issue number1-3
Pages (from-to)175-80
Number of pages6
ISSN0014-2999
Publication statusPublished - 22.06.2001

Research areas and keywords

  • Adrenergic beta-Antagonists
  • Benzopyrans
  • Calcium
  • Carbazoles
  • Dose-Response Relationship, Drug
  • Ethanolamines
  • Female
  • Heart Ventricles
  • Humans
  • Male
  • Metoprolol
  • Middle Aged
  • Myocardial Contraction
  • Propanolamines
  • Ventricular Function

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