Takanashi H, Itoh Z
Department of Pharmacology, Chugai Pharmaceutical Co., Ltd., Shizuoka, Japan.
Jpn J Pharmacol. 1991 Nov;57(3):447-51. doi: 10.1254/jjp.57.447.
The gastric antisecretory activity of 15(R)-15-methylprostaglandin E2 (arbaprostil) was compared with that of natural prostaglandin (PG) E2 in Pavlov pouch dogs. Arbaprostil significantly inhibited pentagastrin- and food-stimulated gastric secretion when it was administered directly into the pouch at a dose of 10-30 micrograms/pouch and 30-300 micrograms/pouch, respectively. Natural PGE2, however, was inactive up to 1000 micrograms/pouch. The data indicate that arbaprostil is a potent, long-acting orally active antisecretory drug that may be useful for the treatment of peptic ulcer disease.
在巴甫洛夫小胃犬中,比较了15(R)-15-甲基前列腺素E2(阿巴前列素)与天然前列腺素(PG)E2的胃抗分泌活性。当分别以10 - 30微克/小胃和30 - 300微克/小胃的剂量直接注入小胃时,阿巴前列素能显著抑制五肽胃泌素和食物刺激引起的胃酸分泌。然而,高达1000微克/小胃的天然PGE2却无活性。这些数据表明,阿巴前列素是一种强效、长效的口服活性抗分泌药物,可能对消化性溃疡疾病的治疗有用。