Inhibition of calcium influx in thrombin-stimulated platelets by SIN-1, an activator of soluble guanylate cyclase

J Cardiovasc Pharmacol. 1989:14 Suppl 11:S106-10.

Abstract

A previous study revealed that elevation of platelet cyclic GMP induced by a pharmacological activator of soluble guanylate cyclase, 3-morpholinosydnonimine (SIN-1), induced a major inhibition of Ca2+ influx caused by thrombin, as detected by monitoring the fluorescence of the Ca2+ indicator quin-2. In contrast, activation of phospholipase C as well as Ca2+ mobilization presumably promoted by inositol-1,4,5-trisphosphate was less affected by SIN-1 treatment. In the present study, the effects of SIN-1 on Ca2+ influx have been investigated in more detail using platelets loaded with millimolar concentrations of quin-2. Under these conditions, Ca2+ entry from the medium into the platelet cytoplasm could be followed either by detecting fluorescence quenching by Mn2+ or by determination of 45Ca2+ uptake. Both events were inhibited by SIN-1 in a dose-dependent manner. Furthermore, the inhibition of 45Ca2+ uptake and of fluorescence increase observed in the presence of extracellular Ca2+ displayed remarkably parallel dose-response curves, suggesting that elevation of cyclic GMP brought about by SIN-1 inhibits the opening of "receptor-operated channels" whose precise nature remains to be determined.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biological Transport
  • Blood Platelets / metabolism*
  • Calcium / metabolism*
  • Cyclic GMP / biosynthesis
  • Enzyme Activation / drug effects
  • Fluorescence
  • Guanylate Cyclase / metabolism
  • Humans
  • In Vitro Techniques
  • Molsidomine / analogs & derivatives*
  • Molsidomine / pharmacology
  • Solubility / drug effects
  • Thrombin / pharmacology*
  • Vasodilator Agents / pharmacology*

Substances

  • Vasodilator Agents
  • linsidomine
  • Molsidomine
  • Thrombin
  • Guanylate Cyclase
  • Cyclic GMP
  • Calcium