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European Heart Journal 1990 11(4):323-327;
Copyright © 1990 by the European Society of Cardiology.
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© 1990 The European Society of Cardiology

The effect of xamoterol in failing human myocardium

R. H. G. SCHWINGER, M. BÖHM and E. ERDMANN

Medizinische Klinik I der Universität München München, F.R.G.

Received 10 April 1989; revised 10 July 1989; .

correspondence to Prof: E. Erdmann, Universität München, Medizinische Klinik I, Marchiomnistrasse 15, D-8000 München 70, F.R.G.

Abstract

As the dual pharmacological action of partial ß1-adrenoceptor agonists should improve left ventricular function while also protecting the myocardium against excessive sympathetic stimulation they may be useful in the treatment of heart failure. Therefore, we studied the pharmacological effects of xamoterol (Corwin, ICl 118, 587), a compound with mixed agonist and antagonistic properties at cardiac ß-adrenoceptors in electrically driven human papillary muscle strips from failing human hearts. Specimens were obtained from patients with different grades of myocardialfailure who underwent mitral valve replacement (NYHA II-III) or heart transplantation (NYHA IV). Xamoterol (0.0001-10.0 µmol 1–1) produced only negative inotropic effects, as measured by changes in isometric force of contraction in diseased human papillary muscle strips. However, isoprenaline (0.0001-10 µmol l–1) and ouabain (0.01-0.3 µmol 1–1) enhanced force of contraction in the same hearts. Prestimulation with noradrenaline (3 µmol l–1) augmented the negative inotropic effect of xamoterol. It is concluded that xamoterol exerts primarily ß-adrenoceptor antagonistic activity in the failing human myocardium

Key Words: Xamoterol • positive inotropic agent • ß-adrenoceptor • heart failure • human myocardium


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