Abstract
1. Cultured brain capillary endothelial cells of the rat respond to endothelin-1 (ET-1) by an increased activity of the Na+,K+,2Cl-, cotransporter and a mobilization of intracellular Ca2+ stores. 2. Calyculin A (1-30 nM), but not okadaic acid, sensitizes up to 100 fold the Na+,K+,2Cl- cotransporter to the action of ET-1. 3. Calyculin A (30 nM) does not modify the binding properties of ET-1 to ETA receptors. 4. Calyculin A (30 nM) inhibits ET-1 induced intracellular Ca2+ mobilization. 5. It is concluded that inhibition of protein phosphatase 1 selectively modifies the repertoire of intracellular actions of ET-1 and favours actions that are unrelated to the phospholipase C signalling cascade.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Brain / cytology
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Brain / drug effects*
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Calcium / metabolism
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Capillaries / cytology
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Capillaries / drug effects
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Carrier Proteins / metabolism
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Cells, Cultured
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Endothelin Receptor Antagonists
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Endothelins / antagonists & inhibitors
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Endothelins / pharmacology*
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Endothelium, Vascular / cytology
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Endothelium, Vascular / drug effects*
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Marine Toxins
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Oxazoles / pharmacology*
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Peptides, Cyclic / pharmacology
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Phosphoprotein Phosphatases / antagonists & inhibitors
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Protein Phosphatase 1
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Rats
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Receptors, Endothelin / drug effects
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Rubidium Radioisotopes
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Sodium-Potassium-Chloride Symporters
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Sodium-Potassium-Exchanging ATPase / metabolism
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Vasoconstrictor Agents / pharmacology*
Substances
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Carrier Proteins
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Endothelin Receptor Antagonists
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Endothelins
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Marine Toxins
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Oxazoles
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Peptides, Cyclic
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Receptors, Endothelin
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Rubidium Radioisotopes
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Sodium-Potassium-Chloride Symporters
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Vasoconstrictor Agents
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calyculin A
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Phosphoprotein Phosphatases
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Protein Phosphatase 1
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Sodium-Potassium-Exchanging ATPase
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cyclo(Trp-Asp-Pro-Val-Leu)
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Calcium