使用竞争性缓激肽拮抗剂Lys-Lys-[Hyp2, Thi5,8, DPhe7]-Bk（B4148）减轻大鼠内毒素休克时动脉血压的下降。

Attenuation of arterial blood pressure fall in endotoxin shock in the rat using the competitive bradykinin antagonist Lys-Lys-[Hyp2, Thi5,8, DPhe7]-Bk (B4148).

作者信息

Weipert J, Hoffmann H, Siebeck M, Whalley E T

机构信息

Abteilung für Klinische Chemie, University of Munich, FRG.

出版信息

Br J Pharmacol. 1988 Jun;94(2):282-4. doi: 10.1111/j.1476-5381.1988.tb11526.x.

DOI:10.1111/j.1476-5381.1988.tb11526.x

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1853989/

Abstract

The selective competitive bradykinin (Bk) antagonist, B4148 (Lys-Lys-[Hyp2, Thi5,8, DPhe7]-Bk) infused at 100 micrograms kg-1 min-1 into rats produced a significant inhibition of the hypotensive effect of Bk and had no effect against acetylcholine-induced responses. In a rat model of endotoxin shock, the fall in mean arterial blood pressure in response to an intravenous injection of lipopolysaccharide from E. coli was significantly attenuated by the same infusion of B4148 compared to controls. These findings suggest that kinins are involved in the hypotensive response to endotoxin shock in rats. The development of potent Bk antagonists offers a new experimental approach for evaluating the role of kinins in this and other disease states and potential therapy in such disorders.

摘要

选择性竞争性缓激肽（Bk）拮抗剂B4148（Lys-Lys-[Hyp2, Thi5,8, DPhe7]-Bk）以100微克/千克·分钟-1的速度注入大鼠体内，可显著抑制Bk的降压作用，而对乙酰胆碱诱导的反应无影响。在内毒素休克大鼠模型中，与对照组相比，相同剂量的B4148注入可显著减轻静脉注射大肠杆菌脂多糖后平均动脉血压的下降。这些发现表明，激肽参与了大鼠对内毒素休克的降压反应。强效Bk拮抗剂的开发为评估激肽在这种及其他疾病状态中的作用以及此类疾病的潜在治疗提供了一种新的实验方法。

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[Activation of the kallikrein-kinin system by endotoxin in the experimental shock model of the rat].[内毒素在大鼠实验性休克模型中对激肽释放酶-激肽系统的激活作用]

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