Ishihara K, Ichikawa T, Komuro Y, Ohara S, Hotta K
Department of Chemistry, School of Medicine, Kitasato University, Kanagawa, Japan.
Arzneimittelforschung. 1994 Jul;44(7):827-30.
The effect of leminoprazole ((+-)-2-[[2-(isobutyl-methylamino)benzyl]sulfinyl]-1H-benzimidazol e, NC-1300-O-3, CAS 104340-86-5), a new compound being developed as an inhibitor of the gastric mucosal proton pump (H+,K(+)-ATPase), on gastric mucus secretion was studied by a biochemical method measuring the gastric mucin content in rats. Oral administration of leminoprazole (30 mg/kg) strongly inhibited the hemorrhagic lesions induced by 60% ethanol containing 0.15 mol/l HCl (acid-ethanol) administered 1 h later. Leminoprazole significantly inhibited the acid-ethanol-induced reduction of the mucin content in the surface mucosa including the mucus gel layer, but no significant effect could be obtained on the reduction of mucin present in the deep layer of the corpus and antral mucosa. Leminoprazole given to rats not treated with acid ethanol accelerated the secretion of deep mucosal mucus and increased significantly the content of soluble mucus which was recovered from the gastric luminal contents to about 200% of control, but failed to produce any significant change in the mucus content present in the surface mucosal and the mucus gel layers. The effect of leminoprazole on gastric mucus secretion might contribute to healing the peptic ulcer diseases and may be involved in the cytoprotective mechanism of this drug.
雷米拉唑（（±）-2-[[2-（异丁基-甲基氨基）苄基]亚磺酰基]-1H-苯并咪唑，NC-1300-O-3，CAS 104340-86-5）是一种正在研发的新型胃黏膜质子泵（H⁺，K⁺-ATP酶）抑制剂，本研究采用生化方法测定大鼠胃黏液含量，探讨其对胃黏液分泌的影响。口服雷米拉唑（30mg/kg）能强烈抑制1小时后给予的含0.15mol/l HCl的60%乙醇（酸-乙醇）诱导的出血性损伤。雷米拉唑显著抑制酸-乙醇诱导的包括黏液凝胶层在内的表面黏膜中黏蛋白含量的降低，但对胃体和胃窦黏膜深层中黏蛋白的降低无显著影响。给未用酸乙醇处理的大鼠服用雷米拉唑可促进深层黏膜黏液的分泌，并使从胃腔内容物中回收的可溶性黏液含量显著增加，达到对照的约200%，但对表面黏膜和黏液凝胶层中的黏液含量未产生任何显著变化。雷米拉唑对胃黏液分泌的作用可能有助于消化性溃疡疾病的愈合，且可能参与该药物的细胞保护机制。
