Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
Graier, WF; Groschner, K; Schmidt, K; Kukovetz, WR.
SK&F 96365 inhibits histamine-induced formation of endothelium-derived relaxing factor in human endothelial cells.
Biochem Biophys Res Commun. 1992; 186(3):1539-1545
Doi: 10.1016/S0006-291X(05)81582-7
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- Führende Autor*innen der Med Uni Graz
- Graier Wolfgang
- Co-Autor*innen der Med Uni Graz
- Groschner Klaus
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- Abstract:
- Formation of endothelium-derived relaxing factor (EDRF) strictly correlates with the intracellular free Ca2+ ([Ca2+]i) concentration. We now demonstrate that the histamine-induced rise in [Ca2+]i of human umbilical vein endothelial cells is mostly due to activation of a membrane current which allows Ca2+ entry. This membrane current is sensitive to the novel inhibitor of agonist-induced Ca2+ entry, SK&F 96365, which blocked the histamine-induced sustained rise in [Ca2+]i, as well as 45Ca2+ uptake and membrane currents. Inhibition of the above cellular responses to histamine was accompanied by a considerable reduction of EDRF formation and release. Thus biosynthesis and release of EDRF from human umbilical vein endothelial cells significantly depend on agonist-induced Ca2+ entry involving receptor-operated Ca(2+)-permeable channels which can be blocked by SK&F 96365.
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