Glimepiride is a sulfonylurea which inhibit KATP with IC50 of 3.0 nM in pancreatic β-cells with fewer cardiac actions. It is used in the treatment of type 2 diabetes mellitus.
Glimepiride (Hoe 490) is a new sulfonylurea. After oral administration of Hoe 490 to rabbits, blood glucose was lowered 3.5 times more than after glibenclamide (HB 419) and after intravenous administration, 2.5 times more. The more rapid decrease in blood glucose in the dog after oral administration of glimepiride was accompanied by a correspondingly earlier and higher plasma insulin increase[3]. Glimepiride is a second-generation sulfonylurea that stimulates pancreatic β cells to release insulin. It can also be combined with other antihyperglycemic agents, including metformin and insulin, in patients who are not adequately controlled by sulfonylureas alone[4]. Glimepiride decreased extracellular Aβ40 and Aβ42 levels. The effect of glimepiride on reduction of Aβ40 generation was mediated by downregulation of β-site APP-cleaving enzyme 1 (BACE1) mRNA and protein expression, and by suppression of BACE1 activity[5].
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