Satoh Y, Satoh H, Honda F
Jpn J Pharmacol. 1980 Oct;30(5):689-99. doi: 10.1254/jjp.30.689.
The inhibitory effect of sulpiride on dopamine receptors was investigated in the exocrine pancreas of dogs anesthetized with pentobarbital and with the stomach ligated at the pylorus. All test substances were given intravenously. Dopamine, acetylcholine, histamine and secretin produced a dose-related increase in pancreatic juice secretion, though the dose-effect curves of these secretagogues differed in shape. Epinephrine, norepinephrine, isoproterenol, methamphetamine and serotonin had no secretagogue effects. The effects of acetylcholine and histamine were inhibited by atropine and cimetidine, respectively. The effect of dopamine was blocked by haloperidol, but not by atropine, cimetidine, phentolamine and propranolol. These results suggest that dopamine acts on specific dopamine receptors related to the exocrine pancreatic secretion. Haloperidol had no effect on the effects of acetylcholine and histamine, but did inhibit the secretin-induced secretion, though the inhibitory effect was to a lesser extent than on the dopamine response. Sulpiride and chlorpromazine also suppressed dose-dependently the dopamine-induced secretion. The inhibitory activity of sulpiride was almost the same as that of haloperidol, and 12 times more potent than that of chlorpromazine. Sulpiride was found to be a potent dopamine antagonist in the canine exocrine pancreas.
在戊巴比妥麻醉且幽门处结扎胃的犬的外分泌胰腺中，研究了舒必利对多巴胺受体的抑制作用。所有受试物质均通过静脉注射给药。多巴胺、乙酰胆碱、组胺和促胰液素可使胰液分泌呈剂量相关增加，尽管这些促分泌剂的剂量-效应曲线形状不同。肾上腺素、去甲肾上腺素、异丙肾上腺素、甲基苯丙胺和5-羟色胺没有促分泌作用。乙酰胆碱和组胺的作用分别被阿托品和西咪替丁抑制。多巴胺的作用被氟哌啶醇阻断，但不受阿托品、西咪替丁、酚妥拉明和普萘洛尔的影响。这些结果表明多巴胺作用于与外分泌胰腺分泌相关的特定多巴胺受体。氟哌啶醇对乙酰胆碱和组胺的作用没有影响，但确实抑制了促胰液素诱导的分泌，尽管其抑制作用程度小于对多巴胺反应的抑制。舒必利和氯丙嗪也剂量依赖性地抑制多巴胺诱导的分泌。舒必利的抑制活性与氟哌啶醇几乎相同，比氯丙嗪强12倍。舒必利被发现是犬外分泌胰腺中一种有效的多巴胺拮抗剂。
