Description
Tolbutamide-d
9 is intended for use as an internal standard for the quantification of tolbutamide by GC- or LC-MS. Tolbutamide is an inhibitor of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel K
ir6.2 (IC
50 = 4.9 μM). It is selective for SUR1/K
ir6.2 over SUR2A/K
ir6.2 and SUR2B/K
ir6.2 channels (IC
50s = 85 and 88 μM, respectively). Tolbutamide increases glucose-induced insulin secretion and calcium influx in isolated mouse pancreatic islets.
In vivo, tolbutamide (80 mg/kg) reduces blood glucose levels in a mouse model of diabetes induced by streptozotocin (STZ; ). Formulations containing tolbutamide have been used in the treatment of type 2 diabetes.
Chemical Properties
White Solid
Uses
Labelled Tolbutamide (T535150). An antidiabetic, used as a hypoglycemic agent in veterinary medicine.
References
[1] PETER PROKS. Sulfonylurea stimulation of insulin secretion.[J]. Diabetes, 2002, 51 Suppl 3: S368-76. DOI:
10.2337/diabetes.51.2007.s368[2] NOBUYOSHI ISHIYAMA Jean C H Magalie A Ravier. Dual mechanism of the potentiation by glucose of insulin secretion induced by arginine and tolbutamide in mouse islets.[J]. American journal of physiology. Endocrinology and metabolism, 2006, 290 3: E540-9. DOI:
10.1152/ajpendo.00032.2005[3] CLAUS RERUP Finn T. Streptozotocin- and alloxan-diabetes in mice[J]. European journal of pharmacology, 1969, 7 1: Pages 89-96. DOI:
10.1016/0014-2999(69)90169-1
