二苄胺对胃酸分泌的体外阻断作用及其组胺拮抗剂的保护作用。

Dibenamine blockade on gastric acid secretion in vitro and its protection by histamine antagonists.

作者信息

Watanabe K, Goto Y

出版信息

Eur J Pharmacol. 1975 Feb;30(2):133-9. doi: 10.1016/0014-2999(75)90091-6.

Abstract

Experiments to protect the histamine receptor against dibenamine blockade were carried out to elucidate the pharmacological characteristics of the H2-histamine receptor system for gastric acid secretion in isolated bullfrog gastric mucosa. Dibenamine alone (5 times 10-minus 5 g/ml) irreversibly blocked both basal and histamine-stimulated acid secretion. However, when the preparation was treated with dibenamine in combination with histamine (1 times 10-minus 5 g/ml) irreversibly blocked both basal and histamine-stimulated acid secretion. However, when the preparation was treated with dibenamine in combination with histamine (1 times 10-minus 5 g/ml), the acid secretory response to histamine was restored after washing out dibenamine. Burimamide, an H2-receptor antagonist, also protected the histamine sensitivity against dibenamine blockade in the concentration of 1 times 10-minus 4 g/ml. Diphenhydramine and pyribenzamine were also protected with histamine receptor against dibenamine blockade. The acid secretion induced by the action of histamine on the diphenhydramine-protected receptor was antagonized by diphenhydramine as well as burimamide.

摘要

为阐明分离的牛蛙胃黏膜中组胺H2受体系统对胃酸分泌的药理学特性，进行了保护组胺受体免受双苄胺阻断的实验。单独使用双苄胺（5×10⁻⁵g/ml）可不可逆地阻断基础胃酸分泌和组胺刺激的胃酸分泌。然而，当制剂用双苄胺与组胺（1×10⁻⁵g/ml）联合处理时，在洗去双苄胺后，对组胺的胃酸分泌反应得以恢复。H2受体拮抗剂布立马胺在浓度为1×10⁻⁴g/ml时也能保护组胺敏感性免受双苄胺阻断。苯海拉明和吡苄明对组胺受体也有保护作用使其免受双苄胺阻断。组胺作用于苯海拉明保护的受体所诱导的胃酸分泌，可被苯海拉明以及布立马胺拮抗。