NCIt definition : Sulfonamide urea derivatives with antihyperglycemic activity. Sulphonylurea antidiabetic
agents bind to sulfonylurea receptor type 1 (SUR1), the subunit of ATP-sensitive inwardly-rectifier
potassium (IKATP) channels on the membranes of pancreatic beta cells, thereby blocking
the inward current flow (influx) of positively charged K ions into the cell. This
results in tonic membrane depolarization, and induces a calcium ion influx through
voltage-sensitive calcium channels; increased intracellular calcium ion levels trigger
exocytosis of insulin-containing granules. This eventually induces secretion of insulin.
The IKATP channels found in pancreatic islets are complexes of four IKATP 6.2 and
four SUR1 subunits. In addition, some sulfonylureas of larger molecular size may increase
the sensitivity of peripheral tissues to insulin mediated through peroxisome proliferator-activated
receptor gamma (PPARgamma).; Sulfonamide urea derivatives with antihyperglycemic activity. Sulphonylurea antidiabetic
agents bind to sulfonylurea receptor type 1 (SUR1), the subunit of ATP-sensitive inwardly-rectifier
potassium (IKATP) channels on the membranes of pancreatic beta cells, thereby blocking
the inward current flow (influx) of positively charged K ions into the cell. This
results in tonic membrane depolarization, and induces a calcium ion influx through
voltage-sensitive calcium channels; increased intracellular calcium ion levels trigger
exocytosis of insulin-containing granules. This eventually induces secretion of insulin.
The IKATP channels found in pancreatic islets are complexes of four IKATP 6.2 and
four SUR1 subunits. In addition, some sulfonylureas of larger molecular size may increase
the sensitivity of peripheral tissues to insulin mediated through peroxisome proliferator-activated
receptor gamma (PPARgamma).;