Hypoglycemic Activity of Valeramide,4-Dimethylamino-N-methyl-2,2-Diphenyl-,Hydrochloride. ∗

Summary

Valeramide, 4-dimethylamino-N-methyl-2,2-diphenyl-, hydrochloride (U-6420) was found to be about 4 times more potent than tolbutamide in lowering blood sugars of fasted intact rats. Although U-6420 was active in depressing blood sugars of adrenalectomized rats, the response was not dose-related, as was the case with tolbutamide. Since hydrocortisone or epinephrine still increased blood sugars of U-6420-treated adrenalectomized rats, it was concluded that the mechanism of hypoglycemic action was not due to inhibition of the metabolic effects of adrenal hormones. It was also found that U-6420 did not lower blood sugars of alloxan diabetic or eviscerate rats, nor increase oxidation of glucose U-C¹⁴ by fasted intact rats. It was concluded from these studies that the mechanism of action of U-6420 was not like that of the sulfonylureas, biguanides, or insulin. The most probable mechanism was that of decreasing glucose output by the liver.