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首页> 外文期刊>Life sciences >A dopamine D3 receptor agonist, 7-hydroxy-N,N-di-n-propyl-2-aminotetralin, reduces gastric acid and pepsin secretion and experimental gastric mucosal injury in rats.
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A dopamine D3 receptor agonist, 7-hydroxy-N,N-di-n-propyl-2-aminotetralin, reduces gastric acid and pepsin secretion and experimental gastric mucosal injury in rats.

机译：多巴胺D3受体激动剂7-羟基-N，N-二-正丙基-2-氨基四氢萘减少大鼠胃酸和胃蛋白酶的分泌以及实验性胃粘膜损伤。

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摘要

Dopamine D1/DA1 agonists are associated with significant gastroprotective and antisecretory effects. The new dopamine DA3 agonist, 7-hydroxy-N,N-di-n-propyl-2-aminotetralin (7-OHDPAT), possesses neural and behavioral properties that are similar to those of DA1 agonists. In the present experiments, the effects of 7-OHDPAT on gastric acid secretion in conscious and anaesthetized rats, on restraint stress-induced gastric mucosal injury and on gastric adherent mucus levels were examined. 7-OHDPAT (2.5, 5.0 and 10.0 mg/kg) reduced significantly basal gastric acid secretion in conscious rats (66%, 92% and 78% inhibition, respectively). 7-OHDPAT also reduced significantly gastric acid and pepsin secretion in pylorus-ligated rats. 7-OHDPAT reduced stress-induced gastric mucosal injury at doses of 1.0, 5.0 and 10.0 mg/kg. Gastric adherent mucus was preserved only at the 5.0 mg/kg dose. Neither pretreatment with the DA1 antagonist, SCH23390, nor with the DA2 antagonist, eticlopride, affected 7-OHDPAT-induced reductions in gastric secretion or gastric mucosal injury. Although dopamine DA3 receptors exhibit greater amino acid sequence homology with DA2 receptors than with DA1 receptors, the possibility nevertheless exists that some of the gastrointestinal actions of dopamine and its agonists--both anti-secretory and gastroprotective--may be exerted through activation of DA3 receptors.
机译：多巴胺D1 / DA1激动剂与显着的胃保护和抗分泌作用有关。新的多巴胺DA3激动剂7-羟基-N，N-二-正丙基-2-氨基四氢萘（7-OHDPAT）具有与DA1激动剂相似的神经和行为特性。在本实验中，研究了7-OHDPAT对清醒和麻醉大鼠胃酸分泌，束缚应激诱导的胃粘膜损伤和胃黏附黏液水平的影响。 7-OHDPAT（2.5、5.0和10.0 mg / kg）明显降低了清醒大鼠的基础胃酸分泌（分别为66％，92％和78％抑制）。 7-OHDPAT还显着降低了幽门结扎大鼠的胃酸和胃蛋白酶分泌。 7-OHDPAT以1.0、5.0和10.0 mg / kg的剂量减轻了应激引起的胃粘膜损伤。仅以5.0 mg / kg的剂量保存胃黏附粘液。用DA1拮抗剂SCH23390预处理，或用DA2拮抗剂艾替洛德都没有影响7-OHDPAT诱导的胃液分泌或胃粘膜损伤的减少。尽管多巴胺DA3受体与DA2受体的氨基酸序列同源性高于DA1受体，但仍有可能通过激活DA3发挥多巴胺及其激动剂的某些胃肠道作用（抗分泌和保护胃）受体。

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