Inatomi N, Hirata T, Inada I, Satoh H, Sino A, Maki Y
Arzneimittelforschung. 1985;35(10):1553-9.
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.
研究了新合成的化合物5-乙酰基螺[苯并呋喃-2(3H),1'-环丙烷]-3-酮（AG 629）对各种实验性诱导溃疡的影响。以25 - 100 mg/kg的剂量口服或十二指肠内给予AG 629，可抑制大鼠的水浸应激性溃疡、运动性溃疡、 Shay溃疡、吲哚美辛和乙酰水杨酸（ASA）诱导的胃溃疡以及吲哚美辛诱导的小肠溃疡，抑制豚鼠组胺诱导的胃溃疡和犬ASA诱导的胃溃疡，不过它对大鼠半胱胺诱导的十二指肠溃疡无效。以6.3 - 25 mg/kg的剂量口服AG 629，每日两次，可显著促进大鼠乙酸或热可的松诱导的胃溃疡以及乙酸诱导的十二指肠溃疡的愈合。AG 629（25 - 100 mg/kg十二指肠内给药）可抑制幽门结扎大鼠的胃酸和胃蛋白酶分泌以及空气扩张大鼠胃刺激引起的胃酸分泌，而该化合物不影响组胺、五肽胃泌素、卡巴胆碱或2-脱氧-D-葡萄糖刺激的胃酸分泌。本研究表明，AG 629对各种溃疡具有预防和治疗作用。该药物的抗溃疡作用似乎主要通过增加黏膜抵抗力介导，其次通过抗分泌活性介导。
