Research Area: Metabolic Disease
Biological Activity:
Gliclazide (Diamicron) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 ± 30 nM. Gliclazide (Diamicron) binds to sulfonylurea receptors on the surface of the Beta islet cells found in the pancreas. This binding effectively closes the K+ ion channels. This decreases the efflux of potassium from the cell which leads to the depolarization of the cell. This causes voltage dependent Ca2+ ion channels to open increasing the Ca2+ influx. The calcium can then bind to and activate calmodulin which in turn leads to exocystosis of insulin vesicles leading to insulin release. Gliclazide is used for control of hyperglycemia in gliclazide-responsive diabetes mellitus of stable, mild, non-ketosis prone, maturity-onset or adult type. Gliclazide (Diamicron) is used when diabetes cannot be controlled by proper dietary management and exercise or when insulin therapy is not appropriate. [1][2][3]References on Gliclazide (Diamicron)[1] Diabetologia. , 2001 Aug, 44(8):1019-25[2] http://en.wikipedia.org/wiki/Gliclazide, , [3] Diabetes., 2009 Oct, 58(10):2419-24 |