Kagoshima M, Kodaira H, Shimada H
Department of Clinical Pharmacology, School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
Nihon Yakurigaku Zasshi. 1994 Nov;104(5):379-89. doi: 10.1254/fpj.104.379.
We examined the effects of FRG-8813, a new histamine H2-receptor antagonist with potent antisecretory activity, on gastric mucus in male SD rats (7w). In this study, the effects of FRG-8813 (1, 3, 10 mg/kg), given orally twice a day for 7 days, were investigated by histochemical and biochemical methods in comparison with those of cimetidine (CM, 30 mg/kg) and famotidine (FM, 1 mg/kg) in the fundic gland area (F. area) and pyloric gland area (P. area). In the histochemical study by alcian blue (pH 2.5)-PAS (AB-PAS) or high iron diamine-alcian blue (HID-AB) staining, the CM group showed a significant decrease in PAS and tended to show decreases in HID-AB positive mucus and mucous gel layer in the F. area; the FM group also showed a decrease in AB positive mucus in the P. area. On the other hand, the AB-PAS and HID-AB positive mucus of the FRG-8813 group were not affected. In the biochemical study, FRG-8813 increased the gastric mucosal hexose, hexosamine and sialic acid composing the mucus in a dose-dependent manner in the F. area. These results suggest that FRG-8813 does not cause a decrease in gastric mucus, unlike CM or FM, and it may be able to promote mucus secretion through increasing the mucous component in the F. area.
我们研究了新型组胺H2受体拮抗剂FRG - 8813（具有强大的抗分泌活性）对雄性SD大鼠（7周龄）胃黏液的影响。在本研究中，通过组织化学和生物化学方法，比较了FRG - 8813（1、3、10毫克/千克，每日口服两次，共7天）与西咪替丁（CM，30毫克/千克）和法莫替丁（FM，1毫克/千克）在胃底腺区（F.区）和幽门腺区（P.区）的作用。在阿尔新蓝（pH 2.5）-过碘酸希夫（AB - PAS）或高铁二胺 - 阿尔新蓝（HID - AB）染色的组织化学研究中，CM组在F.区的PAS显著降低，且HID - AB阳性黏液和黏液凝胶层有降低趋势；FM组在P.区的AB阳性黏液也有减少。另一方面，FRG - 8813组的AB - PAS和HID - AB阳性黏液未受影响。在生物化学研究中，FRG - 8813在F.区以剂量依赖方式增加了构成黏液的胃黏膜己糖、氨基己糖和唾液酸。这些结果表明，与CM或FM不同，FRG - 8813不会导致胃黏液减少，并且它可能能够通过增加F.区的黏液成分来促进黏液分泌。
