Ishihara K, Komuro Y, Nishiyama N, Yamasaki K, Hotta K
Department of Biochemistry, School of Medicine, Kitasato University, Sagamihara, Japan.
Arzneimittelforschung. 1992 Dec;42(12):1462-6.
The effect of rebamipide (2-(4-chlorobenzoylamino)-3-[2 (1H)-quinolinon-4-yl]-propionic acid, OPC-12759, CAS 11911-87-6), an anti-ulcer agent developed to enhance defensive factors in the gastric mucosa, on gastric mucus secretion was studied by a newly developed biochemical method to measure the gastric mucus glycoprotein content in rats. 1 h after intraperitoneal administration, rebamipide did not produce a significant change in the intramucosal mucus contents (surface mucosal layer and deep mucosal layers of corpus and antral regions) but significantly increased the content of soluble mucus, which recovered from the gastric contents, to about 160% of the control value. Since rebamipide has been shown to increase the biosynthesis of prostaglandins, indometacin was administered to the rats prior to rebamipide administration to examine whether the increase in prostaglandin biosynthesis contributes to the rebamipide-induced increase in gastric mucus secretion. The increase in the soluble mucus was not altered by the pretreatment with indometacin, thus indicating that rebamipide per se has a potential to increase the gastric mucus secretion by a mechanism that is not mediated by the endogenous prostaglandins. The effect of rebamipide on the gastric mucus secretion might contribute to heal and to prevent the recurrence of peptic ulcer diseases as well as to maintain the homeostasis of the gastric mucosa.
瑞巴派特(2-(4-氯苯甲酰氨基)-3-[2 (1H)-喹啉酮-4-基]-丙酸,OPC-12759,CAS 11911-87-6)是一种为增强胃黏膜防御因子而研发的抗溃疡药物,本研究采用一种新开发的生化方法测定大鼠胃黏液糖蛋白含量,以研究其对胃黏液分泌的影响。腹腔注射1小时后,瑞巴派特对黏膜内黏液含量(胃体和胃窦区域的表面黏膜层和深层黏膜层)无显著影响,但显著增加了从胃内容物中回收的可溶性黏液含量,使其达到对照值的约160%。由于已证明瑞巴派特可增加前列腺素的生物合成,因此在给予瑞巴派特之前先给大鼠注射吲哚美辛,以检查前列腺素生物合成的增加是否有助于瑞巴派特诱导的胃黏液分泌增加。吲哚美辛预处理并未改变可溶性黏液的增加,这表明瑞巴派特本身具有通过一种不由内源性前列腺素介导的机制增加胃黏液分泌的潜力。瑞巴派特对胃黏液分泌的影响可能有助于消化性溃疡疾病的愈合和预防复发,以及维持胃黏膜的稳态。