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rdf:type |
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lifeskim:mentions |
umls-concept:C0021467,
umls-concept:C0021469,
umls-concept:C0086418,
umls-concept:C0216524,
umls-concept:C0225336,
umls-concept:C0244485,
umls-concept:C0596235,
umls-concept:C1527240,
umls-concept:C1550548,
umls-concept:C1555714,
umls-concept:C1704259,
umls-concept:C1705654,
umls-concept:C1705987
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pubmed:issue |
4
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pubmed:dateCreated |
1997-2-18
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pubmed:abstractText |
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.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/8904644-1318033,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8904644-13576452,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8904644-1531101,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8904644-1965707,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8904644-2173565,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8904644-312319,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8904644-7516040,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8904644-7746267,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8904644-7838664,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8904644-7943286,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8904644-8010948,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8904644-8033342,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8904644-8229840,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8904644-8469608
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
0007-1188
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
119
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
702-6
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:8904644-Acetamides,
pubmed-meshheading:8904644-Calcium,
pubmed-meshheading:8904644-Calcium Channels,
pubmed-meshheading:8904644-Cells, Cultured,
pubmed-meshheading:8904644-Endothelium, Vascular,
pubmed-meshheading:8904644-Humans,
pubmed-meshheading:8904644-Ionomycin,
pubmed-meshheading:8904644-Isoquinolines,
pubmed-meshheading:8904644-Membrane Potentials,
pubmed-meshheading:8904644-Thapsigargin
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pubmed:year |
1996
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pubmed:articleTitle |
Inhibition of a store-operated Ca2+ entry pathway in human endothelial cells by the isoquinoline derivative LOE 908.
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pubmed:affiliation |
Institut für Pharmakologie and Toxikologie, Karl-Franzens-Universit?t Graz, Austria.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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