Ichikawa T, Ishihara K, Saigenji K, Hotta K
Department of Biochemistry, Kitasato University School of Medicine, Kanagawa, Japan.
Eur J Pharmacol. 1994 Jan 4;251(1):107-11. doi: 10.1016/0014-2999(94)90451-0.
The effects of the anti-acid secretory agents, cimetidine (N-cyano-N'-methyl-N"-(2-([(5-methyl-1H-imidazol-4-yl)methyl]thio)ethyl) guanidine), ranitidine (N-(2-(((-5-[(dimethylamino)methyl]-2-furanyl)methyl)thio)ethyl)-N'-meth yl- 2-nitro-1,1-ethene-diamine), roxatidine (2-acetoxy-N-(3-[m-(1-piperidinylmethyl)phenoxy]-propyl) acetamide hydrochloride), FRG-8813 (2-(furfurylsulfinyl)-N-(4-[4-(piperidinomethyl)-2-pyridyl]o xy-(z)-2- butenyl)acetamide), omeprazole (5-methoxy-2-([(4-methoxy-3,5-dimethylpyridinyl)methyl]sulfinyl)- 1H-benzimidazole), and NC-1300-O-3 (2-([2-(isobutylmethylamino)benzyl]sulfinyl)-1H- benzimidazole), on mucin biosynthesis were studied in rat gastric mucosa by using an organ culture technique. [3H]Glucosamine incorporation was stimulated in the corpus region by the histamine H2 receptor antagonists which have a six-membered aromatic ring, roxatidine and FRG-8813, and the new H+,K(+)-ATPase inhibitor, NC-1300-O-3. Thus, these drugs not only inhibit acid secretion but may also promote gastric mucosal protective actions. The present observations also demonstrate that the determination of mucin biosynthesis may be a useful tool for evaluation of mucosal protective activity.
采用器官培养技术，研究了抗酸分泌剂西咪替丁（N-氰基-N'-甲基-N''-(2-([(5-甲基-1H-咪唑-4-基)甲基]硫代)乙基)胍）、雷尼替丁（N-(2-(((-5-[(二甲氨基)甲基]-2-呋喃基)甲基)硫代)乙基)-N'-甲基-2-硝基-1,1-乙烯二胺）、罗沙替丁（2-乙酰氧基-N-(3-[间-(1-哌啶基甲基)苯氧基]-丙基)乙酰胺盐酸盐）、FRG-8813（2-(糠基亚磺酰基)-N-(4-[4-(哌啶甲基)-2-吡啶基]氧基-(Z)-2-丁烯基)乙酰胺）、奥美拉唑（5-甲氧基-2-([(4-甲氧基-3,5-二甲基吡啶基)甲基]亚磺酰基)-1H-苯并咪唑）和NC-1300-O-3（2-([2-(异丁基甲基氨基)苄基]亚磺酰基)-1H-苯并咪唑）对大鼠胃黏膜黏蛋白生物合成的影响。具有六元芳香环的组胺H2受体拮抗剂罗沙替丁和FRG-8813以及新型H⁺,K⁺-ATP酶抑制剂NC-1300-O-3可刺激胃体部[³H]葡萄糖胺的掺入。因此，这些药物不仅抑制胃酸分泌，还可能促进胃黏膜保护作用。本研究结果还表明，测定黏蛋白生物合成可能是评估黏膜保护活性的一种有用工具。
