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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1988-8-8
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pubmed:abstractText |
Azelastine, an orally effective anti-allergic agent, has been demonstrated to inhibit the release of histamine and leukotrienes. This suggests that azelastine might alter the mobilization of intracellular Ca2+. We have examined the effect of azelastine on the change in intracellular free calcium concentration ([Ca2+])i) in guinea pig peritoneal macrophages induced by platelet activating factor (PAF-acether) or N-formylmethionyl-leucyl-phenylalanine (FMLP) using a fluorescent Ca2+ indicator, fura2. PAF-acether raised [Ca2+]i from 89 +/- 4 to 243 +/- 26 nM (n = 15) within 20 s after addition of PAF-acether in the presence of 2 mM EGTA. This indicates that the stimulation of macrophages by PAF-acether induced intracellular mobilization of Ca2+, and pretreatment with azelastine reduced the PAF-acether-induced increase in [Ca2+]i in a dose-dependent manner (IC50 = 16 microM). Azelastine also inhibited the FMLP-induced increase in [Ca2+]i. Furthermore, PAF-acether and FMLP both caused the release of prostaglandin E2 from macrophages, and pretreatment with azelastine reduced the PGE2 release dose dependently (IC50 = 10 microM). These results suggest that azelastine inhibits the release of Ca2+ from intracellular storage sites induced by PAF-acether or FMLP, and that this effect possibly causes reduction in the release of PGE2 from the cells.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Calcium,
http://linkedlifedata.com/resource/pubmed/chemical/Dinoprostone,
http://linkedlifedata.com/resource/pubmed/chemical/Histamine H1 Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Ketotifen,
http://linkedlifedata.com/resource/pubmed/chemical/N-Formylmethionine...,
http://linkedlifedata.com/resource/pubmed/chemical/Phthalazines,
http://linkedlifedata.com/resource/pubmed/chemical/Platelet Activating Factor,
http://linkedlifedata.com/resource/pubmed/chemical/Prostaglandins E,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridazines,
http://linkedlifedata.com/resource/pubmed/chemical/azelastine
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0014-2999
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
22
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pubmed:volume |
148
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
35-41
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pubmed:dateRevised |
2004-12-8
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pubmed:meshHeading |
pubmed-meshheading:2898372-Animals,
pubmed-meshheading:2898372-Calcium,
pubmed-meshheading:2898372-Cells, Cultured,
pubmed-meshheading:2898372-Dinoprostone,
pubmed-meshheading:2898372-Guinea Pigs,
pubmed-meshheading:2898372-Histamine H1 Antagonists,
pubmed-meshheading:2898372-Ketotifen,
pubmed-meshheading:2898372-Macrophages,
pubmed-meshheading:2898372-Male,
pubmed-meshheading:2898372-N-Formylmethionine Leucyl-Phenylalanine,
pubmed-meshheading:2898372-Peritoneal Cavity,
pubmed-meshheading:2898372-Phthalazines,
pubmed-meshheading:2898372-Platelet Activating Factor,
pubmed-meshheading:2898372-Prostaglandins E,
pubmed-meshheading:2898372-Pyridazines
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pubmed:year |
1988
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pubmed:articleTitle |
Effect of azelastine on the intracellular Ca2+ mobilization in guinea pig peritoneal macrophages.
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pubmed:affiliation |
Tsukuba Research Laboratories, Eisai Co., Ltd., Ibaragi, Japan.
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pubmed:publicationType |
Journal Article
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