Glimepiride is a long-acting sulfonylurea that inhibits ATP-sensitive potassium (KATP) channels in pancreatic β-cells (IC50 = 3 nM), which leads to the release of insulin.{25521} At 20 μM, glimepiride has been shown to increase the activity of intracellular insulin receptors and to prevent insulin receptor downregulation during chronic insulin stimulation through a mechanism involving protein kinase C activation.{25523} It has been reported to be less effective at inhibiting nonpancreatic KATP channels, and therefore contributes fewer cardiac actions, compared to earlier generations of sulfonylurea anti-type 2 diabetes treatments.{25522}
产品描述
A long-acting sulfonylurea that inhibits KATP channels in pancreatic β-cells (IC50 = 3 nM), which leads to the release of insulin; increases the activity of intracellular insulin receptors and prevents insulin receptor downregulation during chronic insulin stimulation through a mechanism involving PKC activation
