Specific receptors for endothelin‐3 in cultured bovine endothelial cells and its cellular mechanism of action
Open Access
- 24 April 1990
- journal article
- Published by Wiley in FEBS Letters
- Vol. 263 (2) , 261-264
- https://doi.org/10.1016/0014-5793(90)81388-5
Abstract
Among three endothelin (ET) isopeptides, ET‐3 shows the most potent initial depressor response through the endothelium‐dependent mechanism. We studied the presence of specific binding sites for ET‐3 in cultured bovine endothelial cells (EC) and its cellular mechanism of action. Binding studies revealed the presence of two distinct subclasses of ET‐3 receptors with high and low affinities. ET‐3 dose‐dependently (10−10−10−7 M) increased both intracellular Ca2+ levels ([Ca−2]) and inositol trisphosphate (IP3) formation. The ET‐3‐induced increase in [Ca2+]i was not affected by either removal of extracellular Ca2+ or Ca2+‐channel blockers. These data suggest that ET‐3 induces phosphoinositide breakdown and increase in [Ca2+]i in ECs, possibly resulting from intracellular Ca2+ mobilization, thereby leading to vasodilatation.Keywords
This publication has 12 references indexed in Scilit:
- Two different forms of endothelin receptors in rat lungFEBS Letters, 1989
- Two distinct types of endothelin receptors are present on chick cardiac membranesBiochemical and Biophysical Research Communications, 1989
- High and low affinity binding sites for endothelin on cultured rat glomerular mesangial cellsBiochemical and Biophysical Research Communications, 1989
- The human endothelin family: three structurally and pharmacologically distinct isopeptides predicted by three separate genes.Proceedings of the National Academy of Sciences, 1989
- Rat endothelin is a vasodilator in the isolated perfused mesentery of the ratEuropean Journal of Pharmacology, 1989
- Mediators produced by the endothelial cell.Hypertension, 1988
- Pressor effects of circulating endothelin are limited by its removal in the pulmonary circulation and by the release of prostacyclin and endothelium-derived relaxing factor.Proceedings of the National Academy of Sciences, 1988
- Endothelin stimulates phospholipase C in cultured vascular smooth muscle cellsBiochemical and Biophysical Research Communications, 1988
- Cellular mechanism of action by a novel vasoconstrictor endothelin in cultured rat vascular smooth muscle cellsBiochemical and Biophysical Research Communications, 1988
- A novel potent vasoconstrictor peptide produced by vascular endothelial cellsNature, 1988