Linked Life Data

3525195

Source:http://linkedlifedata.com/resource/pubmed/id/3525195

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
1986-9-16
pubmed:abstractText
Compound UL-DF 9 corresponds to the non-sulfonylurea moiety of gliquidone, a hypoglycaemic sulfonylurea of the second generation. Its effects on the B-cell function were studied in vitro with mouse islets. In the presence of a non-stimulatory concentration of glucose (3 mM), UL-DF 9 decreased 86Rb+ efflux and accelerated 45Ca2+ efflux from islet cells, depolarized the B-cell membrane and induced an electrical activity similar to that triggered by stimulatory concentrations of glucose, and increased insulin release. The changes in 45Ca2+ efflux and insulin release, but not the inhibition of 86Rb+ efflux, were abolished in the absence of Ca2+. In the presence of 10 mM glucose, UL-DF 9 increased 86Rb+ and 45Ca2+ efflux from the islets, augmented the electrical activity in B-cells, and potentiated insulin release. These changes were suppressed by omission of extracellular Ca2+. Qualitatively similar effects were produced by lower concentrations of gliquidone itself. The data suggest that UL-DF 9 and gliquidone decrease the K+ permeability of the B-cell membrane, thereby causing a depolarization which leads to activation of voltage-dependent Ca channels and Ca2+ influx, and thus eventually increase insulin release. Hypoglycaemic sulfonylureas of the second generation therefore seem to contain a second chemical group that interacts with K channels of B-cells as does the sulfonylurea group itself.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
0014-2999
pubmed:author
pubmed:issnType
Print
pubmed:day
27
pubmed:volume
124
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
309-16
pubmed:dateRevised
2011-11-17
pubmed:meshHeading
pubmed:year
1986
pubmed:articleTitle
The non-sulfonylurea moiety of gliquidone mimics the effects of the parent molecule on pancreatic B-cells.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't