SK&F 96365 inhibits histamine-induced formation of endothelium-derived relaxing factor in human endothelial cells.

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.

authors

Graier WF,Groschner K,Schmidt K,Kukovetz WR

doi

10.1016/s0006-291x(05)81582-7

subject

Has Abstract

pub_date

1992-08-14 00:00:00

pages

1539-45

issue

3

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(05)81582-7

journal_volume

186

pub_type

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