Abstract
We studied whether endothelin (ET) isopeptides have any effects on adenylate cyclase activity in cultured bovine endothelial cells (ECs). Both ET-1 and ET-3 dose-dependently inhibited cAMP formation stimulated by forskolin and isoproterenol, although the inhibitory effect of ET-1 was less potent than that of ET-3. In contrast, ET-1 and ET-3 almost equipotently inhibited forskolin-stimulated cAMP formation in bovine EC pretreated with phosphoramidon, a putative ET-1 converting-enzyme inhibitor. These data suggest that endothelial ETB receptors are functionally coupled to adenylate cyclase, possibly via Gi protein.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenylyl Cyclases / metabolism*
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Animals
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Cattle
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Cells, Cultured
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Colforsin / pharmacology
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Cyclic AMP / metabolism
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Endothelin Receptor Antagonists
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Endothelium, Vascular / drug effects
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Endothelium, Vascular / enzymology*
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Endothelium, Vascular / metabolism
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GTP-Binding Proteins / metabolism*
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Glycopeptides / pharmacology
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Isoproterenol / pharmacology
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Nitric Oxide / pharmacology
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Receptors, Endothelin / drug effects
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Receptors, Endothelin / metabolism*
Substances
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Endothelin Receptor Antagonists
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Glycopeptides
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Receptors, Endothelin
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Colforsin
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Nitric Oxide
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Cyclic AMP
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GTP-Binding Proteins
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Adenylyl Cyclases
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Isoproterenol
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phosphoramidon