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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
1989-10-17
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pubmed:abstractText |
The human erythroleukemia (HEL) cell line is a cultured hematopoietic cell line reported to express platelet membrane glycoproteins and alpha-2 adrenergic receptors. The present studies were designed to determine if functional thromboxane A2 (TXA2)/prostaglandin H2 (PGH2) receptors exist in HEL cells. Radioligand binding assays were performed using [125I]PTA-OH, a TXA2/PGH2 receptor antagonist. Scatchard analysis revealed one class of binding sites for 1-PTA-OH with a Kd = 122 +/- 18 nM and maximum binding = 1.7 +/- 0.3 x 10(5) sites/cell. Competition for [125I]PTA-OH binding with the TXA2/PGH2 receptor agonists SQ26655 and U46619 revealed one class of binding sites for SQ26655 with a Kd = 17 nM and two classes of binding sites for for U46619 with a Kd = 45 nM for the high-affinity site and a Kd = 450 nM for the low-affinity site. Competition for [125I]PTA-OH by the steroisomeric TXA2/PGH2 receptor antagonists L657925 and L657926 revealed two classes of binding sites for the more potent L657925 with a Kd = 8 nM for the high-affinity site and a Kd = 400 nM for the low-affinity site whereas L657926 bound to one class of sites with a Kd = 380 nM. Stimulation of the TXA2/PGH2 receptor by SQ26655 and U46619 resulted in concentration-dependent increases in [Ca++], as measured by FURA-2 fluorescence, with EC50 values of 28 +/- 2 and 149 +/- 32 nM, respectively. I-PTA-OH, L657925 and L657926 antagonized this response to U46619 with IC50 values similar in rank potency to that seen in the binding studies.(ABSTRACT TRUNCATED AT 250 WORDS)
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pubmed:grant | |
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/Dimethyl Sulfoxide,
http://linkedlifedata.com/resource/pubmed/chemical/Prostaglandin Endoperoxides...,
http://linkedlifedata.com/resource/pubmed/chemical/Prostaglandin H2,
http://linkedlifedata.com/resource/pubmed/chemical/Prostaglandins H,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Prostaglandin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Thromboxane,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Thromboxane A2...,
http://linkedlifedata.com/resource/pubmed/chemical/Thromboxane A2,
http://linkedlifedata.com/resource/pubmed/chemical/Thromboxane B2
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0022-3565
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
250
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
923-7
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:2528631-Calcium,
pubmed-meshheading:2528631-Cell Differentiation,
pubmed-meshheading:2528631-Dimethyl Sulfoxide,
pubmed-meshheading:2528631-Humans,
pubmed-meshheading:2528631-Leukemia, Erythroblastic, Acute,
pubmed-meshheading:2528631-Prostaglandin Endoperoxides, Synthetic,
pubmed-meshheading:2528631-Prostaglandin H2,
pubmed-meshheading:2528631-Prostaglandins H,
pubmed-meshheading:2528631-Radioligand Assay,
pubmed-meshheading:2528631-Receptors, Prostaglandin,
pubmed-meshheading:2528631-Receptors, Thromboxane,
pubmed-meshheading:2528631-Receptors, Thromboxane A2, Prostaglandin H2,
pubmed-meshheading:2528631-Thromboxane A2,
pubmed-meshheading:2528631-Thromboxane B2,
pubmed-meshheading:2528631-Tumor Cells, Cultured
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pubmed:year |
1989
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pubmed:articleTitle |
Human erythroleukemia cells express functional thromboxane A2/prostaglandin H2 receptors.
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pubmed:affiliation |
Department of Cell and Molecular Pharmacology and Experimental Therapeutics, Medical University of South Carolina, Charleston.
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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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