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舒必利(一种多巴胺D2受体拮抗剂)对大鼠胃和十二指肠的抗溃疡活性。

Gastric and duodenal anti-ulcer activity of sulpiride, a dopamine D2 receptor antagonist, in rats.

作者信息

Desai J K, Parmar N S

机构信息

Department of Pharmacology, B.V. Patel Pharmaceutical Education, Research & Development Centre, Ahmedabad, India.

出版信息

Agents Actions. 1994 Oct;42(3-4):149-53. doi: 10.1007/BF01983482.

Abstract

The gastric and duodenal anti-ulcer activity of sulpiride, a dopamine D2 receptor antagonist, was studied on various types of experimentally induced ulcers in rats, viz., pylorus ligation and water immersion + restraint stress-induced gastric ulcers, gastric mucosal damage induced by nonsteroidal anti-inflammatory drugs and reserpine, and duodenal ulcers induced by cysteamine hydrochloride. It has been found to possess significant anti-ulcer activity against all these models. In 19 h pylorus ligated rats, it significantly reduced the gastric secretion, increased the fucose and sialic acid concentration of the gastric juice and reduced its protein content, thus increasing the total carbohydrate:protein (TC/PR) ratio. These results suggest that the antisecretory and gastric mucosal barrier strengthening effects of sulpiride may be responsible for its anti-ulcer activity. A central component also appears to be involved in its anti-ulcer action against water immersion + restraint stress model. The results of this study provide a rationale for its beneficial effect seen in the therapy of peptic ulcer disease.

摘要

对多巴胺D2受体拮抗剂舒必利的胃和十二指肠抗溃疡活性进行了研究,该研究针对大鼠多种类型的实验性诱导溃疡,即幽门结扎和水浸+束缚应激诱导的胃溃疡、非甾体抗炎药和利血平诱导的胃黏膜损伤,以及盐酸半胱胺诱导的十二指肠溃疡。已发现它对所有这些模型均具有显著的抗溃疡活性。在幽门结扎19小时的大鼠中,它显著减少胃液分泌,增加胃液中岩藻糖和唾液酸浓度,并降低其蛋白质含量,从而提高总碳水化合物:蛋白质(TC/PR)比值。这些结果表明,舒必利的抗分泌和增强胃黏膜屏障作用可能是其抗溃疡活性的原因。中枢成分似乎也参与其对水浸+束缚应激模型的抗溃疡作用。本研究结果为其在消化性溃疡疾病治疗中所见的有益效果提供了理论依据。

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