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缓激肽B2受体拮抗剂艾替班特对小鼠实验性溃疡性结肠炎发展的影响。

Effect of icatibant, a bradykinin B2 receptor antagonist, on the development of experimental ulcerative colitis in mice.

作者信息

Arai Y, Takanashi H, Kitagawa H, Wirth K J, Okayasu I

机构信息

Project Management & Planning Department, Drug Innovation & Approval, Hoechst Marion Roussel Ltd., Tokyo, Japan.

出版信息

Dig Dis Sci. 1999 Apr;44(4):845-51. doi: 10.1023/a:1026694732602.

Abstract

Dextran sulfate sodium-induced colitis in mice has been recognized as a model for human ulcerative colitis. Using this model, we carried out a study on the preventive effect of Icatibant, a bradykinin B2 receptor antagonist previously called HOE 140, on the development of colitis. Subcutaneous administration of Icatibant (0.3 or 1.5 mg/kg) significantly suppressed shortening of the large intestine and worsening of the general health. Oral administration of Icatibant (50 mg/kg) significantly suppressed shortening of the large intestine, the onset of diarrhea, and worsening of the general health. In addition, the oral treatment significantly inhibited the development of colitis that was observed histopathologically. These results indicate a role of BK in the development of dextran sulfate sodium-induced colitis in mice, and suggest that BK could be important in human ulcerative colitis.

摘要

硫酸葡聚糖钠诱导的小鼠结肠炎已被公认为人类溃疡性结肠炎的模型。利用该模型,我们开展了一项关于依卡替班(一种先前称为HOE 140的缓激肽B2受体拮抗剂)对结肠炎发展预防作用的研究。皮下注射依卡替班(0.3或1.5毫克/千克)可显著抑制大肠缩短和整体健康状况恶化。口服依卡替班(50毫克/千克)可显著抑制大肠缩短、腹泻发作和整体健康状况恶化。此外,口服治疗显著抑制了组织病理学观察到的结肠炎发展。这些结果表明缓激肽在硫酸葡聚糖钠诱导的小鼠结肠炎发展中起作用,并提示缓激肽在人类溃疡性结肠炎中可能很重要。

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