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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3-4
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pubmed:dateCreated |
1990-1-25
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pubmed:abstractText |
H1-receptor reserves in guinea-pig left atria, trachea and pig coronary arteries were calculated by the use of phenoxybenzamine (Pba), a beta-haloalkylamine that irreversibly blocks the H1-receptor response to histamine or 2-(2-pyridyl)-ethylamine (PEA). Equieffective concentrations of the H1-agonist in the absence (A) and presence (A') of Pba were evaluated from concentration-response curves. By plotting the reciprocal values 1/A versus 1/A' the amount of H1-receptors not occupied by the agonist was calculated. The size of the H1-receptor reserve could be estimated by comparison of the receptor occupation with the corresponding effect. Furthermore, the dissociation constants for histamine, PEA, Pba and the pD'2-values for Pba were determined for the different tissues. 5% and 6% H1-receptor occupation is necessary to achieve a half maximal contraction of the trachea with the agonists histamine and PEA, respectively. Only 0.5% H1-receptor occupation is needed for the half maximal positive inotropic effect of histamine in left atria, while 5.5% of the H1-receptors have to be occupied using PEA as an agonist in this tissue. In the coronary artery of the pig 50% of the maximal contraction can be achieved by stimulation of 15.1% of the H1-receptors with histamine.
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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/2-(2-aminoethyl)pyridine,
http://linkedlifedata.com/resource/pubmed/chemical/Histamine,
http://linkedlifedata.com/resource/pubmed/chemical/Phenoxybenzamine,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Histamine H1
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0065-4299
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
28
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
218-23
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:2596374-Animals,
pubmed-meshheading:2596374-Coronary Vessels,
pubmed-meshheading:2596374-Guinea Pigs,
pubmed-meshheading:2596374-Histamine,
pubmed-meshheading:2596374-Muscle, Smooth,
pubmed-meshheading:2596374-Muscle Contraction,
pubmed-meshheading:2596374-Myocardial Contraction,
pubmed-meshheading:2596374-Myocardium,
pubmed-meshheading:2596374-Phenoxybenzamine,
pubmed-meshheading:2596374-Pyridines,
pubmed-meshheading:2596374-Receptors, Histamine H1,
pubmed-meshheading:2596374-Swine,
pubmed-meshheading:2596374-Trachea
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pubmed:year |
1989
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pubmed:articleTitle |
H1-receptor reserves in guinea-pig left atria, trachea and pig coronary artery as identified by phenoxybenzamine.
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pubmed:affiliation |
Institute of Pharmacology, University of Düsseldorf, FRG.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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