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Cytoprotective and antisecretory effects of 11-deoxy-13,14-didehydro-16(s)-methyl PGE2 methylester (FCE 20700).

Abstract
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.
AuthorsC Arrigoni, B Mizzotti, D Toti, F Faustini, R Ceserani
JournalProstaglandins, leukotrienes, and medicine (Prostaglandins Leukot Med) Vol. 15 Issue 1 Pg. 79-89 (Jul 1984) ISSN: 0262-1746 [Print] Scotland
PMID6591214 (Publication Type: Journal Article)
Chemical References
  • Anti-Ulcer Agents
  • Prostaglandins E, Synthetic
  • Ethanol
  • FCE 20700
  • Dinoprostone
  • Indomethacin
Topics
  • Animals
  • Anti-Ulcer Agents
  • Diarrhea (chemically induced)
  • Dinoprostone (analogs & derivatives)
  • Ethanol (antagonists & inhibitors)
  • Gastric Juice (metabolism)
  • Indomethacin (antagonists & inhibitors)
  • Intestines
  • Male
  • Peptic Ulcer (prevention & control)
  • Prostaglandins E, Synthetic (pharmacology)
  • Rats
  • Secretory Rate (drug effects)
  • Stomach Ulcer (chemically induced)
  • Stress, Physiological (complications)

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