Electrophysiological evaluation of the beta-blocking properties and direct membrane effects of l-moprolol and its enantiomer d-moprolol

Arch Int Pharmacodyn Ther. 1989 May-Jun:299:200-9.

Abstract

The electrophysiological and beta-blocking properties of l- and d-moprolol have been studied in sheep cardiac Purkinje fibers. l-Moprolol (0.3-100 nM) dose-dependently antagonized the inotropic (ED50 = 1.2 +/- 0.4 nM) and chronotropic (ED50 = 5.8 +/- 0.6 nM) effects of isoprenaline. d-Moprolol (0.3-100 nM) was fully devoid of beta-blocking properties under the same experimental conditions. Both isomers had the same electrophysiological profile: they did not influence action potential characteristics, contractility and normal automaticity up to 1 microM. On the whole, l-moprolol appears to be a potent beta-blocker, exerting membrane depressant effects only at a concentration 2000 times higher than those exerting effective beta-blockade.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Action Potentials / drug effects
  • Adrenergic beta-Antagonists / pharmacology*
  • Animals
  • Electrophysiology*
  • Heart / drug effects
  • Heart / innervation
  • Heart Rate / drug effects
  • In Vitro Techniques
  • Membranes / drug effects
  • Myocardial Contraction / drug effects
  • Phenoxypropanolamines
  • Potassium Chloride / pharmacology
  • Propanolamines / pharmacology*
  • Purkinje Fibers / drug effects
  • Sheep
  • Stereoisomerism

Substances

  • Adrenergic beta-Antagonists
  • Phenoxypropanolamines
  • Propanolamines
  • Potassium Chloride
  • moprolol