Trivulzio S, Colombo R, Rossoni G, Caironi E
Department of Pharmacology, Chemotherapy and Medical Toxicology, University of Milan.
Pharmacol Res Commun. 1988 Nov;20(11):975-82. doi: 10.1016/s0031-6989(88)80125-5.
Benzimidazole and some of its derivatives as 4-nitro and 5-nitro-benzimidazoles, 2-amino-, 4-amino- and 5-aminobenzimidazoles have been tested on gastric acid secretion in Shay-rats. Only 5-aminobenzimidazole decreased the gastric secretory process basal or stimulated by betazole. The antisecretory properties of 5-aminobenzimidazole seem to be linked to an anti H2-histamine activity, since this compound depresses the amplitude of contractions of guinea pig isolated auricle stimulated by betazole. The antisecretive activity appears to be associated to a definite distance between the amino group and the imidazolyl nitrogen, since it appears only when the amino function is located in position 5 of the benzimidazole structure.
苯并咪唑及其一些衍生物，如4-硝基和5-硝基苯并咪唑、2-氨基-、4-氨基-和5-氨基苯并咪唑，已在沙伊大鼠身上进行胃酸分泌测试。只有5-氨基苯并咪唑能降低基础胃酸分泌过程或由倍他唑刺激引起的胃酸分泌。5-氨基苯并咪唑的抗分泌特性似乎与抗H2组胺活性有关，因为该化合物能抑制由倍他唑刺激的豚鼠离体耳廓收缩幅度。抗分泌活性似乎与氨基和咪唑基氮之间的特定距离有关，因为只有当氨基官能团位于苯并咪唑结构的5位时才会出现这种活性。
