A New High-Potency Antidiabetic Sulfonylurea [N-(1-hexahydro-1-azepinyl)-N′- p -tolyl-sulfonylurea]. ∗

Abstract

Summary

U-17835 ([N-(1-hexahydro-1-azepinyl)-N′-p-tolyl-sulfonylurea]), a new blood sugar lowering sulfonylurea, was 4-6 times more active than tolbutamide in intact rats and 4 times more active in adrenalectomized rats. At equipotent doses it was not longer acting than tolbutamide in intact rats. Normal human subjects showed U-17835 to be 6-7 times more effective than tolbutamide in lowering blood sugar after a single dose. In 3 diabetic patients, U-17835, given for 8 weeks, was found to be 5-10 times more active than tolbutamide, and it showed no signs of intolerance. This compound was also better tolerated than tolbutamide in both rats and mice.

The authors wish to express their appreciation to P. M. Jones for conducting the acute toxicity studies.