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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1981-5-21
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pubmed:abstractText |
The action of the non-steroidal antiinflammatory drugs indomethacin, tiaprofenic acid, diclofenac and meclofenamate on vascular and platelet-cyclooxygenases was studied by measuring the arachidonic acid-induced thromboxane A2 (TXA2)-formation of washed human platelets and prostacyclin (PGI2)-formation of bovine coronary artery rings. TXA2 was bioassayed as RCS on rabbit aorta strips, PGI2 in terms of its antiaggregatory activity on ADP-induced aggregation of human platelet-rich plasma. All of the substances studied produced concentration-dependent inhibition of PGI2- and RCS-release. The IC50 [micrometer] in inhibition of RCS-formation was 0.019 for indomethacin, 0.070 for tiaprofenic acid but 44.9 for meclofenamate and 63.2 for diclofenac. The IC50 [micrometer] in inhibition of PGI2-release was 0.42 for diclofenac, 0.63 for indomethacin and 0.99 for tiaprofenic acid. The data suggest (1) high sensitivity of human platelet-cyclooxygenase against indomethacin and tiaprofenic acid, (2) different sequence of the substances studied in inhibiting arachidonic acid-induced TXA2- and PGI2-formation. The possible therapeutic value of selective inhibition of platelets and vascular cyclooxygenases is discussed.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
0028-1298
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
313
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
69-76
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:6782492-Animals,
pubmed-meshheading:6782492-Anti-Inflammatory Agents,
pubmed-meshheading:6782492-Blood Platelets,
pubmed-meshheading:6782492-Cattle,
pubmed-meshheading:6782492-Coronary Vessels,
pubmed-meshheading:6782492-Dose-Response Relationship, Drug,
pubmed-meshheading:6782492-Epoprostenol,
pubmed-meshheading:6782492-Humans,
pubmed-meshheading:6782492-Prostaglandin-Endoperoxide Synthases,
pubmed-meshheading:6782492-Rabbits,
pubmed-meshheading:6782492-Thromboxane A2,
pubmed-meshheading:6782492-Time Factors
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pubmed:year |
1980
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pubmed:articleTitle |
Different sensitivities of prostaglandin-cyclooxygenases in blood platelets and coronary arteries against non-steroidal antiinflammatory drugs.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|