Reference

The pharmacodynamics of two new sulfonylurea derivatives

The pharmacodynamics of two new sulfonylurea derivatives. Haupt, E.; Kuellmer, K. A.; Schoeffling, K. (Zent. Inn. Med., Johann Wolfgang Goethe-Univ., Frankfurt/Main, Ger.). Klin. Wochenschr., 55(14), 695-703 (German) 1977. CODEN: KLWOAZ. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) In healthy human subjects, the equipotent doses (decreasing blood sugar by 30%) for i.v. administered gliquidone (I) [33342-05-1] and gliflumide (II) [35273-88-2] were 0.10 and 0.12 mg/kg, compared with 7.5 and 0.006 mg/kg for tolbutamide [64-77-7] and glibenclamide [10238-21-8], resp. Following oral administration, the resp. 30% effective doses were 0.30, 0.038, 25, and 0.032 mg/kg, resp. After i.v. administration, the blood glucose decrease corresponded with insulin [9004-10-8] levels. I resembled tolbutamide whereas II resembled glibenclamide in effects on blood glucose and insulin. Differences in insulin secretion after sulfonylurea administration were not obsd. after oral administration.

Binding of hypoglycemic sulfonylureas to an artificial phospholipid bilayer

Binding of hypoglycemic sulfonylureas to an artificial phospholipid bilayer. Deleers, M.; Malaisse, W. J. (Med. Sch., Brussels Univ., Brussels B-1000, Belg.). Diabetologia, 26(1), 55-9 (English) 1984.Several substances with their cas registry numbers 64-77-7 and 21187-98-4 may be metioned in this study. CODEN: DBTGAJ. ISSN: 0012-186X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Hypoglycemic sulfonylureas bind to multilamellar liposomes formed of egg yolk phosphatidylcholine. In this model, both specific and nonspecific components can be characterized by the same criteria as those used in studies performed with natural membranes. The relative ability of different sulfonylureas to inhibit the bonding of 3H-labeled glibenclamide [10238-21-8] or 3H-labeled gliquidone [33342-05-1] to the liposomes parallels their relative potency as insulin [9004-10-8] secretagogs. Apparently, the insertion of hypoglycemic sulfonylureas into the phospholipid domain of the B cell membrane could represent a primary event in the mechanism by which these agents stimulate insulin release. .