A neuropeptide with diverse biological activities
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 (KATP) 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 KATP 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)
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