Glimepiride-d
4 is intended for use as an internal standard for the quantification of glimepiride by GC- or LC-MS. Glimepiride is a long-acting sulfonylurea that inhibits ATP-sensitive potassium (K
ATP) channels in pancreatic β-cells (IC
50 = 3 nM), which leads to the release of insulin.
1 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.
2 It has been reported to be less effective at inhibiting nonpancreatic K
ATP channels, and therefore contributes fewer cardiac actions, compared to earlier generations of sulfonylurea anti-type 2 diabetes treatments.
3
1. Song, D.K., and Ashcroft, F.M. Glimepiride block of cloned β-cell, cardiac and smooth muscle KATP channels Br. J. Pharmacol. 133(1),193-199(2001).
2. Hribal, M.L., D'Alfonso, R., Giovannone, B., et al. The sulfonylurea glimepiride regulates intracellular routing of the insulin-receptor complexes through their interaction with specific protein kinase C isoforms Mol. Pharmacol. 59(2),322-330(2001).
3. Mocanu, M.M., Maddock, H.L., Baxter, G.F., et al. Glimepiride, a novel sulfonylurea, does not abolish myocardial protection afforded by either ischemic preconditioning or diazoxide Circulation 103(25),3111-3116(2001).
