Glybuzole

Glybuzole (Desaglybuzole) is an orally effective hypoglycemic agent. Glybuzole promotes insulin secretion by pancreatic β cells and inhibits glucagon secretion by pancreatic α cells. Glybuzole reduces blood glucose levels as well as arginine-stimulated plasma glucagon levels. Glybuzole can be used in diabetes-related research^[1][2][3]. In Vitro:Glybuzole (4-40 μg/mL; 24 h) binds to human serum albumin (HSA) with a binding constant of 15.6 μM^[2]. In Vivo:Glybuzole (100 mg; intra-arterial; over 10 minutes) in anesthetized mongrel dogs significantly reduces blood glucose, stimulates pancreatic insulin secretion, and suppresses pancreatic glucagon secretion^[1].
Glybuzole (50-100 mg/kg; p.o.; single dose, 29 consecutive days) reduces blood glucose in normal male Wistar rats, with a plasma half-life of 7 hours after a single 50 mg/kg dose, and is primarily excreted in feces and bile^[2].
Glybuzole (50 mg/kg; p.o.; single dose) has reduced blood glucose-lowering efficacy in male Wistar rats pretreated with phenobarbital, and its plasma half-life is shortened to 4.5 hours after a single 50 mg/kg dose^[2].
Glybuzole (50 mg/kg; p.o.; single dose) has its plasma half-life prolonged to 28 hours after a single 50 mg/kg dose and results in sustained blood glucose reduction in male Wistar rats pretreated with SKF 525A^[2].
Glybuzole (50 mg/kg; p.o.; single dose) has its plasma half-life prolonged to 34 hours after a single 50 mg/kg dose, increases urinary excretion 2.5-fold compared to normal rats, and results in sustained blood glucose reduction in male Wistar rats pretreated with Carbon tetrachloride (HY-Y0298)^[2].
Glybuzole (20-100 mg/kg; p.o., i.v.; single dose) reduces blood glucose levels in normal male rabbits^[2].