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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
1994-7-25
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pubmed:abstractText |
Fructose-2,6-bisphosphate is a potent activator of 6-phosphofructo-1-kinase, a key enzyme in glycolysis. We previously revealed that sulfonylureas stimulate fructose-2,6-bisphosphate production in the rat liver by activating 6-phosphofructo-2-kinase. In the present study, we show that CS-045, a new antidiabetic agent, activated 6-phosphofructo-2-kinase and raised fructose-2,6-bisphosphate levels in dispersed rat hepatocytes. This action was time- and dose-dependent. Ten micromolar CS-045 raised the fructose-2,6-bisphosphate content linearly to the submaximal level in 20 min. Dose dependency was observed in the range of 1-30 microM. Thirty micromolar CS-045 completely reversed the inhibitory effect of 0.1 nM glucagon on fructose-2,6-bisphosphate production. CS-045 activated 6-phosphofructo-2-kinase by decreasing the Km value for the substrate (fructose-6-phosphate) without affecting the Vmax. The combination of suboptimal doses of CS-045 and tolbutamide increased fructose-2,6-bisphosphate content more than that induced by each agent alone. These results indicate that CS-045 may reduce plasma glucose by facilitating glycolysis in the liver.
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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/Chromans,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP,
http://linkedlifedata.com/resource/pubmed/chemical/Fructosediphosphates,
http://linkedlifedata.com/resource/pubmed/chemical/Glucagon,
http://linkedlifedata.com/resource/pubmed/chemical/Thiazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Thiazolidinediones,
http://linkedlifedata.com/resource/pubmed/chemical/Tolbutamide,
http://linkedlifedata.com/resource/pubmed/chemical/fructose 2,6-diphosphate,
http://linkedlifedata.com/resource/pubmed/chemical/troglitazone
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0014-2999
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
21
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pubmed:volume |
254
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
257-62
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8013560-Animals,
pubmed-meshheading:8013560-Chromans,
pubmed-meshheading:8013560-Cyclic AMP,
pubmed-meshheading:8013560-Dose-Response Relationship, Drug,
pubmed-meshheading:8013560-Fructosediphosphates,
pubmed-meshheading:8013560-Glucagon,
pubmed-meshheading:8013560-Liver,
pubmed-meshheading:8013560-Male,
pubmed-meshheading:8013560-Rats,
pubmed-meshheading:8013560-Rats, Wistar,
pubmed-meshheading:8013560-Thiazoles,
pubmed-meshheading:8013560-Thiazolidinediones,
pubmed-meshheading:8013560-Tolbutamide
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pubmed:year |
1994
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pubmed:articleTitle |
CS-045, a new oral antidiabetic agent, stimulates fructose-2,6-bisphosphate production in rat hepatocytes.
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pubmed:affiliation |
Third Department of Internal Medicine, Yamaguchi University School of Medicine, Ube, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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