Cytoprotective and antisecretory effects of 11-deoxy-13,14-didehydro-16(s)-methyl PGE2 methylester (FCE 20700).
A new, chemically stable analogue of PGE2, 11-deoxy-13,14-didehydro-16(S)-methyl PGE2 methylester (FCE 20700) was studied for the prevention of different gastrointestinal ulcers and for the inhibition of basal gastric acid secretion in the rat. The diarrhoea-inducing activity was also investigated. FCE 20700 was more potent than PGE2 in the prevention of stress-induced gastric ulcers (ED50 = 262 and 787 mcg/kg) and indomethacin-induced intestinal ulcers (ED50 = 557 and 4569 mcg/kg), and showed the same potency as PGE2 in the prevention of ethanol (ED50 = 9.2 and 14.8 mcg/kg) and indomethacin-induced gastric ulcers (ED50 = 37.8 and 22.3 mcg/kg). FCE 20700 weakly affects gastric acid secretion with an ED50 of 2385 mcg/kg, showing clear separation of antisecretory activity and gastric antiulcer potency. FCE 20700 does not induce diarrhoea in rats at doses up to 6.25 mg/kg, 10 to 600 times the effective antiulcer doses.
D000818:Animals; D000897:Anti-Ulcer Agents; D003967:Diarrhea / Q000139:chemically induced; D015232:Dinoprostone / Q000031:analogs & derivatives*; D000431:Ethanol / Q000037:antagonists & inhibitors; D005750:Gastric Juice / Q000378:metabolism*; D007213:Indomethacin / Q000037:antagonists & inhibitors; D007422:Intestines; D008297:Male; D010437:Peptic Ulcer / Q000517:prevention & control; D011459:Prostaglandins E, Synthetic / Q000494:pharmacology*; D051381:Rats; D012636:Secretory Rate / Q000187:drug effects; D013276:Stomach Ulcer / Q000139:chemically induced; D013312:Stress, Physiological / Q000150:complications
D000897:Anti-Ulcer Agents; D011459:Prostaglandins E, Synthetic; D000431:Ethanol; C040808:FCE 20700; D015232:Dinoprostone; D007213:Indomethacin