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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1985-3-20
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pubmed:abstractText |
CV-3988, rac-3-(N-n-octadecylcarbamoyloxy)-2-methoxypropyl 2-thiazolioethyl phosphate, is a specific inhibitor of the platelet-activating activity of 1-O-alkyl-2-acetyl-sn-glycero-3-phosphorylcholine (AGEPC or PAFacether). Concentrations of CV-3988 between 10(-8) and 10(-7) M inhibited AGEPC-induced aggregation of washed human platelets in a dose-related manner (IC50 = 2.9 +/- 1.1 X 10(-8) M CV-3988) whereas concentrations of CV-3988 as high as 4 X 10(-6) M did not diminish platelet aggregation by thrombin or adenosine diphosphate. The binding of [3H] AGEPC to platelets was inhibited by CV-3988 in a concentration-dependent manner (IC50 = 6.7 +/- 1.8 X 10(-8) M). Compared to AGEPC, CV-3988 has a 1000-fold lower affinity for the AGEPC receptor. CV-3988 did not stimulate platelet metabolism of AGEPC as assessed by thin-layer chromatographic analysis of [3H] AGEPC extracted from platelet suspensions after four hours of incubation. Thus these studies indicate that CV-3988 inhibits platelet activation by AGEPC by inhibiting binding of AGEPC to its specific platelet receptor.
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pubmed:grant | |
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 |
Jan
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pubmed:issn |
0006-291X
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
16
|
pubmed:volume |
126
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
502-8
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:3970703-Blood Platelets,
pubmed-meshheading:3970703-Dose-Response Relationship, Drug,
pubmed-meshheading:3970703-Humans,
pubmed-meshheading:3970703-Phospholipid Ethers,
pubmed-meshheading:3970703-Platelet Activating Factor,
pubmed-meshheading:3970703-Platelet Aggregation,
pubmed-meshheading:3970703-Thiazoles
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pubmed:year |
1985
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pubmed:articleTitle |
Inhibition of binding of the platelet-activating factor AGEPC to platelets by the AGEPC analog rac-3-(N-n-octadecylcarbamoyloxy)-2-methoxypropyl 2-thiazolioethyl phosphate (CV-3988).
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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