R-α-甲基组胺通过中枢组胺H3受体抑制幽门结扎大鼠的胃酸分泌。
R-alpha-methylhistamine-induced inhibition of gastric acid secretion in pylorus-ligated rats via central histamine H3 receptors.
作者信息
Barocelli E, Ballabeni V, Chiavarini M, Impicciatore M
机构信息
Institute of Pharmacology and Pharmacognosy, University of Parma, Italy.
出版信息
Br J Pharmacol. 1995 Aug;115(7):1326-30. doi: 10.1111/j.1476-5381.1995.tb15044.x.
Abstract
- The effect of central H3 histamine receptor activation on gastric acid and pepsin production has been investigated in pylorus-ligated rats. 2. Intracerebroventricular injections (i.c.v.) of the selective H3 agonist, R-alpha-methylhistamine (0.5-50 nmol per rat) caused a dose-dependent inhibition of gastric acid secretion while intravenous administration (5-500 nmol per rat) was completely ineffective. 3. I.c.v. microinjections of mepyramine, tiotidine and thioperamide (51 nmol per rat), selective antagonists at H1-, H2- and H3-sites respectively, failed to modify the acid secretory response to pylorus ligation. 4. The antisecretory effect of R-alpha-methylhistamine (5 nmol per rat, i.c.v.) was selectively prevented by the H3-blocker, thioperamide (51 nmol per rat, i.c.v.), mepyramine and tiotidine pretreatment being completely inactive. 5. Unlike acid secretion, pepsin production was not significantly affected by all the tested compounds. 6. These findings provide the first pharmacological evidence that the activation of central H3 histamine receptors exerts a negative control in the regulation of gastric acid secretion in conscious pylorus-ligated rats.
摘要
- 已经在幽门结扎的大鼠中研究了中枢H3组胺受体激活对胃酸和胃蛋白酶分泌的影响。2. 向脑室内注射（i.c.v.）选择性H3激动剂R-α-甲基组胺（每只大鼠0.5 - 50 nmol）可引起胃酸分泌的剂量依赖性抑制，而静脉注射（每只大鼠5 - 500 nmol）则完全无效。3. 分别向脑室内微量注射H1、H2和H3位点的选择性拮抗剂美吡拉敏、替丁和硫代哌酰胺（每只大鼠51 nmol），未能改变对幽门结扎的胃酸分泌反应。4. H3阻滞剂硫代哌酰胺（每只大鼠51 nmol，i.c.v.）可选择性地阻止R-α-甲基组胺（每只大鼠5 nmol，i.c.v.）的抗分泌作用，美吡拉敏和替丁预处理则完全无活性。5. 与胃酸分泌不同，所有测试化合物对胃蛋白酶分泌均无显著影响。6. 这些发现提供了首个药理学证据，即中枢H3组胺受体的激活在清醒的幽门结扎大鼠胃酸分泌调节中发挥负性控制作用。
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