rdf:type |
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lifeskim:mentions |
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pubmed:issue |
8
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pubmed:dateCreated |
2004-3-25
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pubmed:abstractText |
In the present study, [ 3H ]-candesartan binding experiments were performed on intact Chinese Hamster Ovary cells transfected with the human AT1 receptor (CHO-AT1 cells). Cells were pre-treated with 0.01mg/ml saponin or filipin. Both pre-treatments resulted in an increased dissociation rate and decreased affinity of the insurmountable non-peptide antagonist [3H ]-candesartan. A similar decrease in affinity was observed for the peptide antagonist Sar1-Ile8 angiotensin II and for other non-peptide antagonists, irrespectively of their degree of insurmountability. A similar discrepancy in [ 3H ]-candesartan binding was earlier observed when comparing intact CHO-AT1 cells and membrane preparations thereof. This similarity is further highlighted by the observations that saponin or filipin no longer affect [ 3H ]-candesartan binding to CHO-AT1 cell membranes and that both agents permeabilise the CHO-AT1 cells. This suggests that the intracellular composition and/or organisation of living cells play an active role with regard to antagonist-AT1 receptor interactions.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
|
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 |
67
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pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
1601-6
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:15041477-Angiotensin II,
pubmed-meshheading:15041477-Angiotensin II Type 1 Receptor Blockers,
pubmed-meshheading:15041477-Animals,
pubmed-meshheading:15041477-Benzimidazoles,
pubmed-meshheading:15041477-Binding, Competitive,
pubmed-meshheading:15041477-CHO Cells,
pubmed-meshheading:15041477-Cricetinae,
pubmed-meshheading:15041477-Drug Interactions,
pubmed-meshheading:15041477-Female,
pubmed-meshheading:15041477-Filipin,
pubmed-meshheading:15041477-Humans,
pubmed-meshheading:15041477-Kinetics,
pubmed-meshheading:15041477-Radioligand Assay,
pubmed-meshheading:15041477-Receptor, Angiotensin, Type 1,
pubmed-meshheading:15041477-Saponins,
pubmed-meshheading:15041477-Tetrazoles,
pubmed-meshheading:15041477-Transfection
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pubmed:year |
2004
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pubmed:articleTitle |
Effect of saponin and filipin on antagonist binding to AT 1 receptors in intact cells.
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pubmed:affiliation |
Department of Molecular and Biochemical Pharmacology, Free University of Brussels (VUB), Pleinlaan 2, 1050 Brussels, Belgium. iverheij@vub.ac.be.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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