Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
33
|
pubmed:dateCreated |
1987-12-29
|
pubmed:abstractText |
Sulfonylureas are powerful hypoglycemic drugs that have been used for decades to treat diabetic patients. This paper describes a 86Rb+ flux technique that permits one to study easily the properties of ATP-modulated K+ channels in RINm5F insulinoma cells. Sulfonylureas inhibit this type of K+ channel under conditions of intracellular ATP depletion. The most potent sulfonylureas (glibenclamide, glipizide, and gliquidone) are acting in the nanomolar range of concentration. Inhibition of the single ATP-modulated K+ channels by low concentrations of sulfonylureas was also observed using the patch-clamp technique. The sulfonylurea receptor has been biochemically identified with [3H]glibenclamide. For 10 different sulfonylureas (or sulfonylurea analogs) there was an excellent correlation between efficacy of blockade of ATP-modulated K+ channels and efficacy of binding to the sulfonylurea receptors using the 3H-ligand.
|
pubmed:commentsCorrections | |
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine Triphosphate,
http://linkedlifedata.com/resource/pubmed/chemical/Glyburide,
http://linkedlifedata.com/resource/pubmed/chemical/Hypoglycemic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Ion Channels,
http://linkedlifedata.com/resource/pubmed/chemical/Potassium,
http://linkedlifedata.com/resource/pubmed/chemical/Rubidium
|
pubmed:status |
MEDLINE
|
pubmed:month |
Nov
|
pubmed:issn |
0021-9258
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
25
|
pubmed:volume |
262
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
15840-4
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:2445740-Adenoma, Islet Cell,
pubmed-meshheading:2445740-Adenosine Triphosphate,
pubmed-meshheading:2445740-Animals,
pubmed-meshheading:2445740-Binding, Competitive,
pubmed-meshheading:2445740-Cell Line,
pubmed-meshheading:2445740-Glyburide,
pubmed-meshheading:2445740-Hypoglycemic Agents,
pubmed-meshheading:2445740-Insulinoma,
pubmed-meshheading:2445740-Ion Channels,
pubmed-meshheading:2445740-Kinetics,
pubmed-meshheading:2445740-Pancreatic Neoplasms,
pubmed-meshheading:2445740-Potassium,
pubmed-meshheading:2445740-Rats,
pubmed-meshheading:2445740-Rubidium
|
pubmed:year |
1987
|
pubmed:articleTitle |
The receptor for antidiabetic sulfonylureas controls the activity of the ATP-modulated K+ channel in insulin-secreting cells.
|
pubmed:affiliation |
Centre de Biochimie du Centre National de la Recherche Scientifique, Nice, France.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|