Hypoglycemic action of 2-[2-(4,5-dihydro-1H-imidazol-2-yl)-1-phenylethyl]pyridine dihydrochloride sesquihydrate (DG-5128), a new hypoglycemic agent.

2-[2-(4,5-Dihydro-1H-imidazol-2-yl)-1-phenylethyl]pyridine dihydrochloride sesquihydrate (GD-5128) is a new hypoglycemic agent structurally unrelated to the known hypoglycemics. It was effective in reducing fasting blood glucose levels in mice, rats, dogs and monkeys at a single oral dose ranging from 5 to 25 mg/kg. DG-5128 was also effective in suppressing hyperglycemia induced by oral and subcutaneous glucose load in mice, rats and monkeys. In addition, it was interesting to find that DG-5128 effectively suppressed glucose-induced and post-prandial hyperglycemia in genetically diabetic mice of AyKK strain which were resistant to the action of tolbutamide, and that it strongly and specifically inhibited adrenaline-induced platelet aggregation. The hypoglycemic activity was not affected by simultaneous administration of other drugs including mefenamate, sulfamonomethoxine, cefazolin, dicoumarol, furosemide and clofibrate. DG-5128 did not cause lactic acidosis in rats even after repeated administration of large doses. These findings suggest usefulness of DG-5128 as a new anti-diabetic agent.