Role of histamine H3 receptors in the regulation of gastric functions.
Role of histamine H3 receptors in the regulation of gastric functions.
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发表时间：
2001-12
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通讯作者：
Gabriella Coruzzi;G. Morini;M. Adami;D. Grandi
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作者：
Gabriella Coruzzi;G. Morini;M. Adami;D. Grandi
本文综述了中枢和外周组胺H3受体在调节胃酸分泌和胃粘膜完整性中的作用。通过外周给予选择性激动剂（R）α-甲基组胺激活H3受体，可减少猫、狗、大鼠和兔的酸分泌，同时增加小鼠的酸分泌。对间接刺激，如2-脱氧-D-葡萄糖，食物或pentagastrin的迷走神经通路或肠嗜铬样（ECL）细胞，但不对组胺或dimaestrin的抗分泌作用。组胺或H3受体激动剂中枢给药后，在大鼠中观察到对酸产生的抑制作用。在清醒的大鼠中，（R）α-甲基组胺灌胃给药可对无水乙醇、盐酸、阿司匹林和应激引起的损伤产生胃保护作用。所涉及的机制似乎与粘液产生增加有关，通过一氧化氮非依赖性机制。中枢给予组胺或其代谢产物N（α）-甲基组胺后，也观察到对乙醇的胃保护作用，表明脑受体参与组胺介导的胃功能作用。
The role of central and peripheral histamine H3 receptors in the regulation of gastric acid secretion and gastric mucosal integrity is reviewed. The activation of H3 receptors by peripheral administration of the selective agonist (R)alpha-methylhistamine reduced acid secretion in cats, dogs, rats and rabbits, while increasing it in mice. The antisecretory effects were observed against indirect stimuli that act on vagal pathways or on enterochromaffin-like (ECL) cells, such as 2-deoxy-D-glucose, food or pentagastrin, but not against histamine or dimaprit. Inhibitory effects on acid production were observed in rats after central administration of histamine or of H3 receptor agonists. In the conscious rat intragastric administration of (R)alpha-methylhistamine caused gastroprotective effects against the damage induced by absolute ethanol, HCl, aspirin and stress. The mechanism involved seems to be related to the increased mucus production, via nitric oxide-independent mechanisms. Gastroprotective effects against ethanol were also observed after central administration of histamine or its metabolite N(alpha)-methylhistamine, suggesting that brain receptors participate the histamine-mediated effects on gastric functions.