Influence of calcium antagonists on heart sarcolemmal (Na+ + K(+)-ATPase

Bratisl Lek Listy. 1991 Mar-Apr;92(3-4):155-8.

Abstract

The effect of calcium entry blocking agents nitrendipine and flunarizine on Mg(2+)-ATPase, (Mg2+ + Na(+)-ATPase, (Na+ + K(+)-ATPase and (Mg2+ + Ca(2+)-ATPase activities was studied. Nitrendipine (1 mumol/l-1) exerted a stimulatory effect on (Mg2+ + Na(+)-ATPase activity. Kinetic analysis of this effect revealed a two-fold rise in Vmax value and lowered Km value for activation of the enzyme by Na+ ions. In concentrations 10(-7) and 10(-5) mol.l-1 flunarizine behaved as a non-specific inhibitor of all sarcolemmal ATPases investigated. Nevertheless, in concentration of 10(-6) mol.l-1 flunarizine inhibited selectively the (Mg2+ + Na(+)-ATPase and (Na+ + K(+)-ATPase activities of myocardial sarcolemma. These observations provided evidence that both flunarizine and nitrendipine, in the concentration 10(-6) mol.l-1, modulate the (Mg2+ + Na(+)-ATPase and (Na+ + K(+)-ATPase activities in cardiac sarcolemma. These side effects of the above drugs particularly that of nitrendipine might have potential physiological relevance.

MeSH terms

  • Adenosine Triphosphatases*
  • Animals
  • Ca(2+) Mg(2+)-ATPase / metabolism
  • Calcium Channel Blockers / pharmacology*
  • Calcium-Transporting ATPases / metabolism
  • Flunarizine / pharmacology
  • Myocardium / enzymology*
  • Myocardium / ultrastructure
  • Nitrendipine / pharmacology
  • Rats
  • Sarcolemma / enzymology*
  • Sodium-Potassium-Exchanging ATPase / metabolism*

Substances

  • Calcium Channel Blockers
  • Nitrendipine
  • Adenosine Triphosphatases
  • Ca(2+) Mg(2+)-ATPase
  • magnesium sodium ATPase
  • Calcium-Transporting ATPases
  • Sodium-Potassium-Exchanging ATPase
  • Flunarizine