Glimepiride-d4

Glimepiride-d₄ 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 (IC₅₀ = 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 channelsBr. 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 isoformsMol. 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 diazoxideCirculation103(25)3111-3116(2001)