Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
Encabo, A; Romanin, C; Birke, FW; Kukovetz, WR; Groschner, K.
Inhibition of a store-operated Ca2+ entry pathway in human endothelial cells by the isoquinoline derivative LOE 908.
Br J Pharmacol. 1996; 119(4):702-706
Doi: 10.1111/j.1476-5381.1996.tb15729.x
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- Führende Autor*innen der Med Uni Graz
- Groschner Klaus
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- Abstract:
- 1. The novel cation channel blocker, LOE 908, was tested for its effects on Ca2+ entry and membrane currents activated by depletion of intracellular Ca2+ stores in human endothelial cells. 2. LOE 908 inhibited store-operated Ca2+ entry induced by direct depletion of Ca2+ stores with 100 nM thapsigargin or 100 nM ionomycin with an EC50 of 2 microM and 4 microM, respectively. 3. LOE 908 did not affect thapsigargin- or ionomycin-induced Ca2+ release from intracellular stores up to concentrations of 3 microM. 4. LOE 908 reversibly suppressed thapsigargin- as well as ionomycin-induced whole-cell membrane currents. 5. The LOE 908-sensitive membrane conductance corresponded to a cation permeability of 5.5 and 6.9 fold selectivity for Ca2+ over K+ in the presence of thapsigargin and ionomycin, respectively. 6. Our results suggest that the isoquinoline, LOE 908 is a novel, potent inhibitor of the store-operated (capacitive) Ca2+ entry pathway in endothelial cells.
- Find related publications in this database (using NLM MeSH Indexing)
- Acetamides - pharmacology
- Calcium - metabolism
- Calcium Channels - drug effects
- Cells, Cultured -
- Endothelium, Vascular - cytology Endothelium, Vascular - drug effects Endothelium, Vascular - metabolism
- Humans -
- Ionomycin - pharmacology
- Isoquinolines - pharmacology
- Membrane Potentials - drug effects
- Thapsigargin - pharmacology
- Find related publications in this database (Keywords)
- endothelial cells
- Ca2+ stores
- Ca2+ entry
- membrane currents
- LOE 908