Inhibition of myocardial K+ channels by bromobenzoyl-methyladamantylamine, an adamantane derivative

János Mészáros, Károly Kelemen, Raisa Markó, V. Kecskeméti, József Szegi

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

The effect of bromobenzoyl-methyladamantylamine (BMA) on transmembrane potentials and contractility of atrial and ventricular myocardium of guinea-pig and cat, as well as on transmembrane ionic currents of the frog atrial trabeculae was studied using conventional glass microelectrode and double sucrose-gap voltage clamp techniques. BMA markedly prolonged the action potential duration, depolarized the cell membrane, reduced the rate of rise of the action potential and exerted a positive inotropic effect on non-clamped myocardial preparations. The drug-induced pacemaker activity in ventricular working muscle of cat. Moreover, BMA antagonized the effects of the K+ channel activator acetylcholine in a dose-dependent manner. BMA was found to induced slow response action potentials in K+-depolarized ventricular myocardium of guinea-pig. In voltage clamp experiments, BMA reduced the outward K+ current but had no effect on either rapid inward Na+ or slow inward Ca2+ currents. The results suggest that BMA is capable of selectively blocking the myocardial K+ channels.

Original languageEnglish
Pages (from-to)151-160
Number of pages10
JournalEuropean Journal of Pharmacology
Volume84
Issue number3-4
DOIs
Publication statusPublished - Oct 22 1982

Fingerprint

Adamantane
Action Potentials
Myocardium
Guinea Pigs
Cats
Microelectrodes
Patch-Clamp Techniques
Anura
Membrane Potentials
Acetylcholine
Glass
Sucrose
Cell Membrane
Muscles
Pharmaceutical Preparations

Keywords

  • Action potential
  • Adamantane
  • Heart
  • K channel blockade
  • Membrane currents
  • Slow responses

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Inhibition of myocardial K+ channels by bromobenzoyl-methyladamantylamine, an adamantane derivative. / Mészáros, János; Kelemen, Károly; Markó, Raisa; Kecskeméti, V.; Szegi, József.

In: European Journal of Pharmacology, Vol. 84, No. 3-4, 22.10.1982, p. 151-160.

Research output: Contribution to journalArticle

Mészáros, János ; Kelemen, Károly ; Markó, Raisa ; Kecskeméti, V. ; Szegi, József. / Inhibition of myocardial K+ channels by bromobenzoyl-methyladamantylamine, an adamantane derivative. In: European Journal of Pharmacology. 1982 ; Vol. 84, No. 3-4. pp. 151-160.
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