抑制bradykinin-induced icatibant人类前臂血管舒张血管,一个强有力的B2-receptor拮抗剂。

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Cockcroft JR Chowienczyk PJ,布雷特,本德N, Ritter JM

抑制bradykinin-induced icatibant人类前臂血管舒张血管,一个强有力的B2-receptor拮抗剂。

Br中国新药杂志。1994年10月,38(4):317 - 21所示。

PubMed ID

7833220 (在PubMed

]

文摘

1。icatibant的影响(D-Arg - [Hyp3、Thi5 D-Tic7, Oic8]缓激肽)的B2-kinin受体拮抗剂,是研究bradykinin-induced人的前臂血管舒张。2。八个健康血压正常的人在增加剂量random-placebo学习控制研究。安慰剂,icatibant(20、50和100毫克公斤增长值)进行双盲。前臂静脉闭塞血流测量的体积描记法在增加剂量肱动脉注入血管舒缓激肽(10 - 3000 ng最低为1)安慰剂或icatibant后60 - 90分钟。3所示。icatibant等离子体浓度下降指数每三个剂量后,最终的测量。消除半衰期计算意味着数据线性回归的25日,27日和29分钟后20、50和100毫克公斤剂量分别。4所示。 Icatibant inhibited the effect of bradykinin (P < 0.001 at each dose of icatibant) in a dose-dependent manner. Bradykinin (100 ng min-1) increased mean blood flow in the infused arm by 238 +/- 31% when infused following placebo, by 112 +/- 21% after icatibant 20 micrograms kg-1, by 71 +/- 14% after icatibant 50 micrograms kg-1 and by 48 +/- 9% after icatibant 100 micrograms kg-1. 5. These results demonstrate that icatibant antagonises B2-receptor mediated vasodilation in human forearm resistance vessels. The findings provide a quantitative basis for future studies of the role of bradykinin in the response to angiotensin converting enzyme inhibitors and in circulatory disease.

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药物

Icatibant