Asagoe K, Murakami M, Kita T
Department of Geriatric Medicine, Faculty of Medicine, Kyoto University, Japan.
Eur J Pharmacol. 1995 Mar 6;275(2):179-84. doi: 10.1016/0014-2999(94)00773-z.
Histamine plays an important role in the control of gastric acid secretion. Recently, chlorinated derivatives of histamine have been identified as having multiple effects on the intestinal tract. The aim of this study was to investigate the role of histamine chloramines on gastric acid secretion. We compared the effects of histamine and histamine chloramines on the histamine H2 receptors in vitro using guinea pigs and on gastric acid secretion in rats. With respect to the effects on histamine H2 receptors, histamine monochloramine showed agonist effects similar to those seen with histamine, but the agonist effects of histamine dichloramine were about half those of histamine. Unlike histamine effects, the histamine H2 receptor agonist effects of histamine monochloramine and histamine dichloramine did not disappear after repeated washout. With respect to the stimulation of gastric acid secretion in vivo, histamine monochloramine was similar to histamine, while the effect of histamine dichloramine was 42.2-52.7% of that of histamine. The recovery time to the basal secretory level after completion of stimulation by histamine chloramines was significantly prolonged compared with histamine. These results suggest that histamine chloramines, which bind strongly with histamine H2 receptors, may delay the termination of gastric acid secretion and increase the burden on the gastric and duodenal mucosa.
组胺在胃酸分泌的调控中发挥着重要作用。近来，已证实组胺的氯化衍生物对肠道具有多种作用。本研究的目的是探究组胺氯胺对胃酸分泌的作用。我们比较了组胺和组胺氯胺在体外对豚鼠组胺H2受体以及在大鼠体内对胃酸分泌的影响。就对组胺H2受体的作用而言，一氯胺组胺显示出与组胺类似的激动剂效应，但二氯胺组胺的激动剂效应约为组胺的一半。与组胺的效应不同，一氯胺组胺和二氯胺组胺的组胺H2受体激动剂效应在反复冲洗后并未消失。就体内对胃酸分泌的刺激而言，一氯胺组胺与组胺相似，而二氯胺组胺的效应为组胺的42.2 - 52.7%。与组胺相比，组胺氯胺刺激完成后恢复到基础分泌水平的时间显著延长。这些结果表明，与组胺H2受体紧密结合的组胺氯胺可能会延迟胃酸分泌的终止，并增加胃和十二指肠黏膜的负担。
