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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1-2
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pubmed:dateCreated |
1990-8-17
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pubmed:abstractText |
In the present study we characterized [3H]-mepyramine binding to rat liver plasma membranes. Binding of [3H]-mepyramine proved to be of high affinity (Kd = 7.7 +/- 0.4 nM) and saturable, resulting in a Bmax-value of 70.4 +/- 9.5 pmol/mg protein. However, displacement studies revealed that this binding site was different from other H1-receptor systems. The two stereoisomers of chlorpheniramine were rather ineffective in displacing [3H]-mepyramine and showed a stereospecificity in favour of the L-isomer. Also several H1-receptor agonists were not potent in displacing [3H]-mepyramine from rat liver plasma membranes. Moreover, the histamine metabolite imidazole-4-acetic acid was about as potent as the H1-agonists, whereas imidazole was even more potent. These data strongly suggest that [3H]-mepyramine labels a non-H1-receptor binding site on the rat liver plasma membrane.
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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 |
Apr
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pubmed:issn |
0065-4299
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
30
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
157-60
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:2371917-Aminopyridines,
pubmed-meshheading:2371917-Animals,
pubmed-meshheading:2371917-Cell Membrane,
pubmed-meshheading:2371917-Kinetics,
pubmed-meshheading:2371917-Liver,
pubmed-meshheading:2371917-Male,
pubmed-meshheading:2371917-Proteins,
pubmed-meshheading:2371917-Pyrilamine,
pubmed-meshheading:2371917-Rats,
pubmed-meshheading:2371917-Rats, Inbred Strains,
pubmed-meshheading:2371917-Receptors, Histamine H1,
pubmed-meshheading:2371917-Stereoisomerism
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pubmed:year |
1990
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pubmed:articleTitle |
Labelling of non-H1-receptor binding sites by [3H]-mepyramine on the rat liver plasma membrane.
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pubmed:affiliation |
Department of Pharmacochemistry, Faculty of Chemistry, Vrije Universiteit, Amsterdam, The Netherlands.
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pubmed:publicationType |
Journal Article,
In Vitro
|