Esplugues J V, Whittle B J
Department of Mediator Pharmacology, Wellcome Research Laboratories, Beckenham, Kent, U.K.
Prostaglandins. 1988 Feb;35(2):137-48. doi: 10.1016/0090-6980(88)90082-2.
The pro-ulcerogenic actions of the thromboxane mimetic, U-46619 on the rat gastric mucosa have been investigated, utilizing a novel technique which allows administration directly into the left gastric artery. Local intra-arterial infusion of U-46619 (100-500 ng/kg/min for 10 min) induced dose-dependent macroscopic damage in both the corpus and antral regions, characterized as vasocongestion, disruption and haemorrhage, with deep penetrating ulcers in the antral mucosa. Vascular congestion, epithelial cell and glandular disruption was observed histologically in both corpus and antral regions. Local intra-arterial infusion of lower doses of U-46619 (25-100 ng/kg/min) significantly disrupted the mucosa in the presence of 10% ethanol in a concentration which itself did not induce macroscopic damage. The damaging actions of U-46619 were substantially reduced by pretreatment with the thromboxane-receptor antagonist, BM 13,177 (5mg/kg i.v.) or 16,16-dimethyl PGE2 (5 micrograms/kg s.c.). These findings support the role of endogenous thromboxane A2 as a local mediator of gastric injury.
利用一种能直接注入胃左动脉的新技术,对血栓素类似物U - 46619对大鼠胃黏膜的促溃疡作用进行了研究。局部动脉内输注U - 46619(100 - 500纳克/千克/分钟,持续10分钟)在胃体和胃窦区域均引起剂量依赖性的肉眼可见损伤,表现为血管充血、组织破坏和出血,胃窦黏膜有深部穿透性溃疡。在组织学上,胃体和胃窦区域均观察到血管充血、上皮细胞和腺体破坏。在存在10%乙醇的情况下,局部动脉内输注较低剂量的U - 46619(25 - 100纳克/千克/分钟)能显著破坏黏膜,而该乙醇浓度本身并不会引起肉眼可见的损伤。血栓素受体拮抗剂BM 13,177(静脉注射5毫克/千克)或16,16 - 二甲基前列腺素E2(皮下注射5微克/千克)预处理可显著减轻U - 46619的损伤作用。这些发现支持内源性血栓素A2作为胃损伤局部介质的作用。