Calcium homeostasis in mouse fibroblast cells: affected by U-73122, a putative phospholipase Cβ blocker, via multiple mechanisms
Autor: | Jacopo Meldolesi, Jeremy P. Grierson |
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Rok vydání: | 1995 |
Předmět: |
Pharmacology
Calcium metabolism Thapsigargin Phospholipase C chemistry.chemical_element Stimulation Fibroblasts Calcium Phospholipase Biology Pyrrolidinones Cell biology Mice chemistry.chemical_compound L Cells chemistry Type C Phospholipases Lysophosphatidic acid Animals Homeostasis Estrenes Intracellular Research Article |
Zdroj: | British Journal of Pharmacology. 115:11-14 |
ISSN: | 0007-1188 |
DOI: | 10.1111/j.1476-5381.1995.tb16312.x |
Popis: | 1. The inhibitory effects of the putative phospholipase C beta inhibitor, U-73122, on ligand-induced and thapsigargin-induced [Ca2+]i transients were investigated in mouse fibroblast cells (the L line). 2. Ca2+ release from intracellular stores was stimulated either by ATP (and also by UTP or ADP) working through the activation of a P2U receptor, or by lysophosphatidic acid, which elicited a more pronounced response. 3. U-73122 inhibited the Ca2+ mobilization produced by all the agonists in a dose-dependent manner, consistent with a mode of action involving phospholipase C inhibition. 4. In addition, however, U-73122 slowed the kinetics of intracellular Ca2+ release induced by the Ca(2+)-ATPase inhibitor, thapsigargin, and reduced the influx of Ca2+ across the plasma membrane, following stimulation of store-dependent influx by the latter. 5. We conclude that U-73122 has multiple sites of action, all of which can lead to a change in Ca2+ homeostasis. Thus, particular caution is recommended when employing this agent and when interpreting the results obtained. |
Databáze: | OpenAIRE |
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