title: Sensitization by calyculin A of brain capillary endothelial cells to endothelin-1.
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.
authors.affiliation: Institut de Pharmacologie Moléculaire et Cellulaire du CNRS, Université de Nice-Sophia Antipolis, Valbonne, France.
authors.forename: P
authors.initials: P
authors.lastname: Vigne
authors.forename: J P
authors.initials: JP
authors.lastname: Breittmayer
authors.forename: C
authors.initials: C
authors.lastname: Frelin
mesh_terms: D000818:Animals; D001921:Brain / Q000166:cytology / Q000187:drug effects*; D002118:Calcium / Q000378:metabolism; D002196:Capillaries / Q000166:cytology / Q000187:drug effects; D002352:Carrier Proteins / Q000378:metabolism; D002478:Cells, Cultured; D065128:Endothelin Receptor Antagonists; D016232:Endothelins / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects*; D008387:Marine Toxins; D010080:Oxazoles / Q000494:pharmacology*; D010456:Peptides, Cyclic / Q000494:pharmacology; D010749:Phosphoprotein Phosphatases / Q000037:antagonists & inhibitors; D054645:Protein Phosphatase 1; D051381:Rats; D017466:Receptors, Endothelin / Q000187:drug effects; D012414:Rubidium Radioisotopes; D028021:Sodium-Potassium-Chloride Symporters; D000254:Sodium-Potassium-Exchanging ATPase / Q000378:metabolism; D014662:Vasoconstrictor Agents / Q000494:pharmacology*
chemical_list: D002352:Carrier Proteins; D065128:Endothelin Receptor Antagonists; D016232:Endothelins; D008387:Marine Toxins; D010080:Oxazoles; D010456:Peptides, Cyclic; D017466:Receptors, Endothelin; D012414:Rubidium Radioisotopes; D028021:Sodium-Potassium-Chloride Symporters; D014662:Vasoconstrictor Agents; C059041:calyculin A; D010749:Phosphoprotein Phosphatases; D054645:Protein Phosphatase 1; D000254:Sodium-Potassium-Exchanging ATPase; C072247:cyclo(Trp-Asp-Pro-Val-Leu); D002118:Calcium