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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
1992-10-9
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pubmed:abstractText |
Carbamyl-platelet-activating factor (1-hexadecyl-2-N-methylcarbamyl-glycero-3-phosphocholine; CPAF) is an analog of platelet-activating factor (PAF) containing an N-methylcarbamyl moiety at the sn-2 position. CPAF was tested for effects on the Raji lymphoblast PAF receptor. Binding studies conducted at 4 degrees C demonstrated specific binding that reached saturation within 60-80 min. Scatchard analysis of CPAF binding data revealed a single class of CPAF binding sites (14,800/cell) with a K = 2.9 +/- 0.9 nM. Competition binding studies with PAF indicated that CPAF has about one-third the potency of native PAF. Unlike PAF, however, CPAF was not significantly metabolized by Raji lymphoblasts at 37 degrees C. CPAF was shown to have PAF-agonistic qualities, since 100 pM to 1 microM CPAF increased free intracellular calcium in a dose-dependent manner. The structurally dissimilar PAF receptor antagonists CV-6209 and alprazolam inhibited the CPAF-induced calcium changes at doses that competed with CPAF binding. Treatment of Raji lymphoblasts with PAF or CPAF (10 pM-1 microM) did not affect spontaneous proliferation, suggesting that the PAF receptor is not involved in the proliferative process in this cell line. These studies demonstrate that CPAF is a metabolically stable lymphoblast PAF receptor agonist that may provide a useful tool in the further elucidation of the role of PAF in lymphocyte function.
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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/1-O-hexadecyl-2-N-methylcarbamylphos...,
http://linkedlifedata.com/resource/pubmed/chemical/Phospholipid Ethers,
http://linkedlifedata.com/resource/pubmed/chemical/Platelet Activating Factor,
http://linkedlifedata.com/resource/pubmed/chemical/Platelet Membrane Glycoproteins,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Cell Surface,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, G-Protein-Coupled,
http://linkedlifedata.com/resource/pubmed/chemical/Tritium,
http://linkedlifedata.com/resource/pubmed/chemical/platelet activating factor receptor
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0192-0561
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
14
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
515-23
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:1325953-Burkitt Lymphoma,
pubmed-meshheading:1325953-Humans,
pubmed-meshheading:1325953-Phospholipid Ethers,
pubmed-meshheading:1325953-Platelet Activating Factor,
pubmed-meshheading:1325953-Platelet Membrane Glycoproteins,
pubmed-meshheading:1325953-Receptors, Cell Surface,
pubmed-meshheading:1325953-Receptors, G-Protein-Coupled,
pubmed-meshheading:1325953-Tritium,
pubmed-meshheading:1325953-Tumor Cells, Cultured
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pubmed:year |
1992
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pubmed:articleTitle |
Binding of carbamyl-platelet-activating factor to the Raji lymphoblast platelet-activating factor receptor.
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pubmed:affiliation |
Department of Pharmacology, Ohio State University College of Medicine, Columbus 43210.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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