Source:http://linkedlifedata.com/resource/pubmed/id/10423180
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
1999-8-5
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pubmed:abstractText |
The present study aimed to investigate endothelin-1 (ET-1) receptors in human and swine cardiomyocytes with binding studies using ET(A) and ET(B) selective receptor antagonists (BMS-182874 and BQ-788, respectively). Cell distribution of mRNA expression for ET(A) and ET(B) subtypes was investigated by in situ hybridization using specific cDNA probes. The 1251-ET-1 binding, which reached equilibrium in about 120 min (Kobs = 0.051+/-0.003 min(-1)), was only partially displaceable by the addition of a large excess of ET-1 (about 15% with a half-life of 20 min). In equilibrium binding studies, 125I-ET-1 had a Kd of 0.43+/-0.08 nM and a maximum binding (Bmax) of 42.8+/-6.6 fmol/mg protein. ET(A) and ET(B) receptors are represented in human and swine cardiomyocytes with an 85:15 ratio as indicated by the biphasic pattern of competition of both BMS-182874 and BQ-788. In situ hybridization studies confirmed that myocytes mainly expressed mRNA for ET(A), whereas expression of mRNA for the ET(B) subtype was documented in non-myocyte cells. These results showed that ET-1 binds with high affinity and poor reversibility to specific receptors, in both human and swine isolated ventricular cardiomyocytes, without significant species differences.
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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 |
Jul
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pubmed:issn |
0006-2952
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
58
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
369-74
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:10423180-Adult,
pubmed-meshheading:10423180-Animals,
pubmed-meshheading:10423180-Binding, Competitive,
pubmed-meshheading:10423180-Heart Ventricles,
pubmed-meshheading:10423180-Humans,
pubmed-meshheading:10423180-In Situ Hybridization,
pubmed-meshheading:10423180-Kinetics,
pubmed-meshheading:10423180-Middle Aged,
pubmed-meshheading:10423180-Myocardium,
pubmed-meshheading:10423180-Receptor, Endothelin A,
pubmed-meshheading:10423180-Receptor, Endothelin B,
pubmed-meshheading:10423180-Receptors, Endothelin,
pubmed-meshheading:10423180-Swine,
pubmed-meshheading:10423180-Ventricular Function, Left
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pubmed:year |
1999
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pubmed:articleTitle |
Endothelin receptors in adult human and swine isolated ventricular cardiomyocytes.
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pubmed:affiliation |
Clinica Medica e Cardiologia, University of Florence, Italy. pa.modesti@dfc.unifi.it
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pubmed:publicationType |
Journal Article
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