Takeuchi K, Ishihara Y, Kunimi H, Okabe S
Agents Actions. 1984 Jun;14(5-6):637-42. doi: 10.1007/BF01978900.
Oral FPL-52694 [5-(2-hydroxypropoxy)-8-propyl-4-oxo-4H-1-benzopyran-2-carboxylic acid Na], a new mast cell stabilizer, dose-dependently inhibited gastric acid secretion but increased the volume and pepsin output in pylorus-ligated rats. Intraduodenal FPL-52694 significantly inhibited all of the volume, acidity, acid output and pepsin output. Concerning the acidity, oral administration of the agent showed much more potent inhibition than intraduodenal administration. Oral FPL-52694 markedly inhibited the development of pylorus-ligated ulcers, water-immersion stress- and aspirin-induced gastric erosions and moderately inhibited the formation of reserpine-induced gastric erosions in rats. Intraduodenal FPL-52694 also inhibited pylorus-ligated ulcers whereas it had no effect on aspirin-induced gastric erosions. Histamine-induced gastric erosions were not affected by oral FPL-52694. These effects of FPL-52694 were almost the same as those of cimetidine, except that cimetidine tended to inhibit histamine-induced gastric erosions. Although the precise mechanism of action of FPL-52694 remains unknown, oral FPL-52694 appears to be a promising agent for the treatment of peptic ulcers.
口服新型肥大细胞稳定剂FPL-52694[5-(2-羟基丙氧基)-8-丙基-4-氧代-4H-1-苯并吡喃-2-羧酸 钠],可剂量依赖性抑制幽门结扎大鼠的胃酸分泌,但增加胃液量和胃蛋白酶分泌量。十二指肠内给予FPL-52694可显著抑制胃液量、酸度、酸分泌量和胃蛋白酶分泌量。关于酸度,口服该药物的抑制作用比十二指肠内给药更强。口服FPL-52694可显著抑制幽门结扎性溃疡、水浸应激和阿司匹林诱导的胃糜烂的形成,并适度抑制利血平诱导的大鼠胃糜烂的形成。十二指肠内给予FPL-52694也可抑制幽门结扎性溃疡,但对阿司匹林诱导的胃糜烂无效。口服FPL-52694对组胺诱导的胃糜烂无影响。FPL-52694的这些作用与西咪替丁几乎相同,只是西咪替丁倾向于抑制组胺诱导的胃糜烂。尽管FPL-52694的确切作用机制尚不清楚,但口服FPL-52694似乎是一种治疗消化性溃疡的有前景的药物。