Sulfonyliminoimidazolidines, a new class of oral hypoglycemic agents. 3. Hypoglycemic activity and mode of action of 1-[p-[2-(crotonylamino)-ethyl]-phenylsulfonyl]-3-cyclohexyl-2-imino- imidazolidine (CGP 11 112).
1-[p-[2-(Crotonylamino)-ethyl]-phenylsulfonyl]-3-cyclohexyl-2-imino- imidazolidine (CGP 11 112) is a representative of a new class of oral hypoglycemic agents. It lowers blood glucose in normal animals and in streptozocin (streptozotocin)-diabetic rats. In normal mice, rats and dogs the hypoglycemic effect is more potent (range 3-30 times) and has a shorter duration than that of tolbutamide. CGP 11 112 increases plasma insulin after oral administration in normal animals and stimulates release of insulin in perifused rat islets in vitro (sulfonylurea-like effect). In streptozocin-diabetic rats CGP 11 112 decreases blood glucose with a potency comparable to that of phenformin. In contrast to phenformin, CGP 11 112 does not increase blood lactate in diabetic rats or inhibit intestinal absorption of glucose. An effect of CGP 11 112 on gluconeogenesis and glycogenolysis could not be demonstrated. It is suggested that the hypoglycemic activity in streptozocin-diabetic rats may be due to stimulation of glucose efflux from the circulation. In vitro, CGP 11 112 inhibits glucose oxidation and lipolysis in isolated rat fat cells.
D000273:Adipose Tissue / Q000187:drug effects; D000315:Adrenalectomy; D000818:Animals; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy; D004285:Dogs; D005260:Female; D005943:Gluconeogenesis / Q000187:drug effects; D006003:Glycogen / Q000378:metabolism; D007004:Hypoglycemic Agents; D007093:Imidazoles / Q000494:pharmacology*; D048289:Imidazolidines; D007328:Insulin / Q000378:metabolism; D000078790:Insulin Secretion; D007408:Intestinal Absorption / Q000187:drug effects; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D051381:Rats; D011919:Rats, Inbred Strains
D007004:Hypoglycemic Agents; D007093:Imidazoles; D048289:Imidazolidines; D007328:Insulin; C038573:1-((4-(2-(crotonylamino)ethyl)phenyl)sulfonyl)-3-cyclohexyl-2-iminoimidazolidine; D006003:Glycogen