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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
1992-7-1
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pubmed:abstractText |
The characteristics of endothelin-1 (ET-1) and endothelin-3 (ET-3) binding, and their relationship to second messenger formation in vitro and vascular effects in vivo were studied in the pig. Specific high-affinity binding sites for [125I]ET-1 and [125I]-ET-3 with extremely slow dissociation rates were demonstrated in membrane preparations from the spleen, lung, kidney and spinal cord. Displacement studies showed that receptor populations with much higher affinity for ET-1 than for ET-3 (ETA type) were present in the spleen and renal arteries, while in the whole kidney and spinal cord, receptor populations with similar affinity for ET-1 and ET-3 were found (ETB type). In the lung both receptor subtypes may be present. The precursor forms big ET-1 and big ET-3 were poor ligands although big ET-1 was more active on the ETA site than big ET-3 on the ETB site. Scatchard analysis revealed linear plots in all tissues studied. Both ET-1 and ET-3 increased formation of inositol phosphates in the lung, while ET-1 but not ET-3 was effective in the spleen. Neither ET-1 nor ET-3 were observed to influence basal or stimulated cyclic AMP formation in lung or spleen. ET-1 caused a much more potent and long-lasting increase in splenic and renal vascular resistance in vivo than did ET-3. On the other hand, ET-1 and ET-3 decreased vascular resistance with almost equal potency in the bronchial circulation.
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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 |
Dec
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pubmed:issn |
0014-2999
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
12
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pubmed:volume |
208
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
313-22
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:1667759-Animals,
pubmed-meshheading:1667759-Binding, Competitive,
pubmed-meshheading:1667759-Binding Sites,
pubmed-meshheading:1667759-Bronchi,
pubmed-meshheading:1667759-Cyclic AMP,
pubmed-meshheading:1667759-Endothelins,
pubmed-meshheading:1667759-Iodine Radioisotopes,
pubmed-meshheading:1667759-Kidney,
pubmed-meshheading:1667759-Kinetics,
pubmed-meshheading:1667759-Lung,
pubmed-meshheading:1667759-Membranes,
pubmed-meshheading:1667759-Phosphatidylinositols,
pubmed-meshheading:1667759-Renal Circulation,
pubmed-meshheading:1667759-Second Messenger Systems,
pubmed-meshheading:1667759-Spinal Cord,
pubmed-meshheading:1667759-Spleen,
pubmed-meshheading:1667759-Swine,
pubmed-meshheading:1667759-Vascular Resistance
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pubmed:year |
1991
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pubmed:articleTitle |
Characteristics of endothelin A and B binding sites and their vascular effects in pig peripheral tissues.
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pubmed:affiliation |
Department of Pharmacology, Karolinska Institutet, Stockholm, Sweden.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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