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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
1991-6-3
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pubmed:abstractText |
The patch-clamp technique was used to examine the tolbutamide-sensitivity of the adenosine 5'-triphosphate (ATP)-dependent K+ channel in mouse pancreatic B-cells. When studied at 37 degrees C in cell-attached membrane patches, this channel had a single-channel conductance of 88 pS and was half-maximally inhibited by 2.2 mumol/l tolbutamide in the presence of 3 mmol/l D-glucose and 10 mumol/l nifedipine. The tolbutamide-induced decrease in the amplitude of the single-channel currents indicated that the membrane potential was sufficiently depolarized for initiation of insulin release by 30 but not by 10 mumol/l of tolbutamide. Using 300 mumol/l diazoxide to open the ATP-dependent K+ channels already closed by 3 mmol/l D-glucose alone, it was demonstrated that initiation of insulin release requires closure of more than 98% of all ATP-dependent K+ channels. In excised inside-out membrane patches, the K+ channel-blocking potency of tolbutamide was maximally enhanced by 0.3 mmol/l adenosine 5'-diphosphate (ADP) at the cytoplasmic side. This ADP effect required the presence of Mg2+. Inhibition of K+ channel activity by ATP, ADP (Mg2(+)-free) or their non-hydrolyzable analogues adenylyl-imidodiphosphate (AMP-PNP) and alpha, beta methylene adenosine 5'-diphosphate (AMP-CP) was not accompanied by enhancement of tolbutamide-sensitivity. The results suggest that cytosolic MgADP controls tolbutamide-sensitivity by interaction with a receptor site not identical with the site mediating channel closure and that this control plays a role in the intact B-cell.
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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 |
Nov
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pubmed:issn |
0028-1298
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
342
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
566-74
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pubmed:dateRevised |
2011-11-17
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pubmed:meshHeading |
pubmed-meshheading:2090953-Action Potentials,
pubmed-meshheading:2090953-Adenosine Triphosphate,
pubmed-meshheading:2090953-Animals,
pubmed-meshheading:2090953-Insulin,
pubmed-meshheading:2090953-Islets of Langerhans,
pubmed-meshheading:2090953-Male,
pubmed-meshheading:2090953-Mice,
pubmed-meshheading:2090953-Mice, Inbred Strains,
pubmed-meshheading:2090953-Potassium Channels,
pubmed-meshheading:2090953-Tolbutamide
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pubmed:year |
1990
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pubmed:articleTitle |
Tolbutamide-sensitivity of the adenosine 5'-triphosphate-dependent K+ channel in mouse pancreatic B-cells.
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pubmed:affiliation |
Institut für Pharmakologie und Toxikologie, Universität Göttingen, Federal Republic of Germany.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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