An antidiabetic sulfonylurea
Glimepiride is a sulfonylurea compound and is used to control blood sugar levels in individuals with type 2 diabetes.
When cultured cells in the presence of a physiological insulin dose and glimepiride (10 μM), 2-deoxyglucose uptake was increased to 186% of control. Glimepiride also increased 2-deoxyglucose uptake in the absence of insulin. At the same time, glimepiride increased the expression of both GLUT1 and GLUT4 to 164% and 148% of control, respectively. These results suggested glimepiride increased cardiac glucose uptake in an insulin-independent pathway [1].
In diabetic-prone (DP) BB rats, Glimepiride (200 mg/kg/day) reduced the incidence of diabetes by 23% compared with the control group [2]. In the hyperinsulinemic hyperglycemic KK-Ay mice, glimepiride reduced blood glucose by 40%, HBA1c by 33% and plasma insulin by 50%. In the absence of insulin, glimepiride caused glucose transport up to 60% and 35% of the maximum insulin response in the rat diaphragm and in 3T3 adipocytes, respectively [3].
参考文献:
[1].? B?hr M, von Holtey M, Müller G, et al. Direct stimulation of myocardial glucose transport and glucose transporter-1 (GLUT1) and GLUT4 protein expression by the sulfonylurea glimepiride. Endocrinology, 1995, 136(6): 2547-2553.
[2].? Pan J, Chan EK, Cheta D, et al. The effects of nicotinamide and glimepiride on diabetes prevention in BB rats. Life Sci, 1995, 57(16): 1525-1532.
[3].? Müller G, Satoh Y, Geisen K. Extrapancreatic effects of sulfonylureas--a comparison between glimepiride and conventional sulfonylureas. Diabetes Res Clin Pract, 1995, 28 Suppl: S115-37.
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