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Predicate | Object |
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rdf:type | |
lifeskim:mentions |
umls-concept:C0021467,
umls-concept:C0021469,
umls-concept:C0023546,
umls-concept:C0026336,
umls-concept:C0032231,
umls-concept:C0034693,
umls-concept:C0034721,
umls-concept:C0086045,
umls-concept:C0205263,
umls-concept:C0220781,
umls-concept:C0225778,
umls-concept:C0444498,
umls-concept:C0527949,
umls-concept:C1289971
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pubmed:issue |
4
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pubmed:dateCreated |
1997-6-27
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pubmed:abstractText |
An intrapleural injection of carrageenan in rats induced LTB4 and LTC4/D4/E4 biosynthesis, exudate formation, and cellular influx in the pleural cavity. An injection of calcium ionophore (A23187, 100 nmol) 16-18 h after carrageenan injection augmented leukotriene biosynthesis and exudate formation, but not cellular influx. The carrageenan-induced pleurisy model modifid by A23187 administration was used to study the oral effect of CGS 23885 (N-hydroxy-N-[(6-phenoxy-2H-1-benzopyran-3-yl)-methyl]urea), a potent 5-lipoxygenase (5-LO) inhibitor, on inflammatory parameters. CGS 23885 dose-dependently (1 to 30 mg/kg) inhibited the enhanced LTB4 and LTC4/D4/E4 (1 to 10 mg/kg) biosynthesis, but had no effect on enhanced exudate formation. An inhibitory effect of CGS 23885 of small magnitude on cellular influx due to carrageenan stimulation was seen at 30 mg/kg. The concentrations of CGS 23885 in the pleural fluid were dose-related, and a positive correlation (r2=0.989) between pleural fluid concentration of LTB4 and CGS 23885 was observed. The results confirm that CGS 23885 is a specific, orally active 5-LO inhibitor which can achieve concentrations in the pleural cavity sufficient to inhibit production of LTB4 and LTC4/D4/E4 in an ongoing inflammatory response.
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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/CGS 23885,
http://linkedlifedata.com/resource/pubmed/chemical/Chromones,
http://linkedlifedata.com/resource/pubmed/chemical/Hydroxylamines,
http://linkedlifedata.com/resource/pubmed/chemical/Leukotriene B4,
http://linkedlifedata.com/resource/pubmed/chemical/Lipoxygenase Inhibitors
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0028-1298
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
355
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
470-4
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:9109363-Animals,
pubmed-meshheading:9109363-Chromones,
pubmed-meshheading:9109363-Disease Models, Animal,
pubmed-meshheading:9109363-Dose-Response Relationship, Drug,
pubmed-meshheading:9109363-Hydroxylamines,
pubmed-meshheading:9109363-Leukotriene B4,
pubmed-meshheading:9109363-Lipoxygenase Inhibitors,
pubmed-meshheading:9109363-Male,
pubmed-meshheading:9109363-Pleurisy,
pubmed-meshheading:9109363-Rats,
pubmed-meshheading:9109363-Rats, Sprague-Dawley
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pubmed:year |
1997
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pubmed:articleTitle |
Inhibition of LTB4 biosynthesis in situ by CGS 23885, a potent 5-lipoxygenase inhibitor, correlates with its pleural fluid concentrations in an experimentally induced rat pleurisy model.
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pubmed:affiliation |
Research Department, Novartis Pharmaceuticals Corporation, Summit, NJ 07901, USA.
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pubmed:publicationType |
Journal Article
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