Effects of 5-acetylspiro[benzofuran-2(3H),1'-cyclopropan]-3-one, a new anti-ulcer agent, on experimental acute and chronic ulcers.
The effects of 5-acetylspiro[benzofuran-2(3H),1'-cyclopropan]-3-one (AG 629), a newly synthesized compound, on various experimentally induced ulcers were investigated. Oral or intraduodenal administration of AG 629 in a dose range of 25-100 mg/kg inhibited water-immersion stress ulcer, exertion ulcer, Shay ulcer, indometacin- and acetylsalicylic acid (ASA)-induced gastric ulcer, and indomethacin-induced small intestinal ulcer in rats, histamine-induced gastric ulcer in guinea pigs, and ASA-induced gastric ulcer in dogs, though it was not effective against cysteamine-induced duodenal ulcer in rats. AG 629 in doses of 6.3-25 mg/kg p.o. twice a day significantly promoted the healing of acetic acid- or thermal-cortisone-induced gastric ulcers and acetic acid-induced duodenal ulcers in rats. AG 629 (25-100 mg/kg i.d.) inhibited the secretion of gastric acid and pepsin in pylorus-ligated rats and the acid secretion stimulated by distension of the rat stomach with air, whereas this compound did not affect acid secretion stimulated by histamine, pentagastrin, carbachol or 2-deoxy-D-glucose. This study shows that AG 629 has both prophylactic and curative effects on various ulcers. The anti-ulcer effect of this agent seems to be mediated primarily by increasing mucosal resistance and secondarily by an antisecretory activity.
D000085:Acetates; D019342:Acetic Acid; D000208:Acute Disease; D000818:Animals; D000897:Anti-Ulcer Agents / Q000494:pharmacology* / Q000627:therapeutic use; D001241:Aspirin; D001572:Benzofurans / Q000494:pharmacology* / Q000627:therapeutic use; D002908:Chronic Disease; D003543:Cysteamine; D004285:Dogs; D004381:Duodenal Ulcer / Q000139:chemically induced / Q000188:drug therapy* / Q000503:physiopathology; D005260:Female; D005744:Gastric Acid / Q000378:metabolism; D006168:Guinea Pigs; D006632:Histamine; D006358:Hot Temperature; D007213:Indomethacin; D008297:Male; D005082:Physical Exertion; D051381:Rats; D011919:Rats, Inbred Strains; D013276:Stomach Ulcer / Q000188:drug therapy* / Q000209:etiology / Q000503:physiopathology; D013315:Stress, Psychological / Q000150:complications
D000085:Acetates; D000897:Anti-Ulcer Agents; D001572:Benzofurans; D003543:Cysteamine; D006632:Histamine; C045902:spizofurone; D019342:Acetic Acid; D001241:Aspirin; D007213:Indomethacin