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Hypoglycemic sulfonylureas represent a group of clinically useful antidiabetic compounds that stimulate insulin secretion from pancreatic beta cells. The molecular mechanisms involved are not fully understood but are believed to involve inhibition of potassium channels sensitive to adenosine triphosphate (KATP channels) in the beta cell membrane, causing membrane depolarization, calcium influx, and activation of the secretory machinery. In addition to these effects, sulfonylureas also promoted exocytosis by direct interaction with the secretory machinery not involving closure of the plasma membrane KATP channels. This effect was dependent on protein kinase C (PKC) and was observed at therapeutic concentrations of sulfonylureas, which suggests that it contributes to their hypoglycemic action in diabetics.

Type

Journal article

Journal

Science

Publication Date

09/02/1996

Volume

271

Pages

813 - 815

Keywords

Animals, Calcium, Cells, Cultured, Cytoplasmic Granules, Electric Conductivity, Exocytosis, Glipizide, Glyburide, Hypoglycemic Agents, Insulin, Islets of Langerhans, Membrane Potentials, Mice, Patch-Clamp Techniques, Protein Kinase C, Sulfonylurea Compounds, Tolbutamide