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[对甲磺酸乙酯对氨基苯甲酰基己酸胍酯(FOY)对激肽生成及纤溶活性的影响]

[Effect of [ethyl p-(6-guanidinohexanoyloxy)benzoate] methanesulfonate (FOY) on kinin formation and fibrinolysis activity].

作者信息

Aishita H, Okegawa T, Akimoto A, Makita T, Shimizu H

出版信息

Nihon Yakurigaku Zasshi. 1975 Jan;71(1):89-99. doi: 10.1254/fpj.71.89.

Abstract

Inibitory effects of [Ethyl p-(6-guanidinohexanoyloxy)benzoate] methanesulfonate (FOY) on kinin formation (in vitro and in vivo) and the fibrinolytic activity (in vivo) were examined and compared with otherinhibitors. Inhibitory effect on kinin forming activity (in vitro) of various enzymes was measured in the guinea pig ileum. FOY and Trasylol inhibited the kinin forming activities of trypsin, pancreas kallikrein and plasma kallikrein. Soybean trypsin inhibitor inhibited kinin like substance was formed in the perfusate when the rat's paw was heated at 46 degrees C. FOY and T-asylol added to the perfusion fluid produced a potent inhibition of the formation of bradykinin-like substance. When administered i.v., FOY and Trasylol did not inhibit the formation of bradykinin-like substance. In the dog, activation of plasmin in the circulatory blood and increase of hemorrhagic tendency were caused by the i.v. administration of human serum plus streptokinase. Such responses were inhibited with a previous i.v. infusion of FOY and t-AMCHA. From the above findings, it may be concluded that FOY has inhibitory effects on kinin formation and fibrinolytic activity.

摘要

研究了甲磺酸盐[对(6-胍基己酰氧基)苯甲酸乙酯](FOY)对激肽形成(体外和体内)和纤溶活性(体内)的抑制作用,并与其他抑制剂进行了比较。在豚鼠回肠中测定了各种酶对激肽形成活性(体外)的抑制作用。FOY和抑肽酶抑制了胰蛋白酶、胰腺激肽释放酶和血浆激肽释放酶的激肽形成活性。当大鼠爪在46℃加热时,大豆胰蛋白酶抑制剂抑制了灌注液中激肽样物质的形成。向灌注液中加入FOY和抑肽酶可有效抑制缓激肽样物质的形成。静脉注射时,FOY和抑肽酶不抑制缓激肽样物质的形成。在狗身上,静脉注射人血清加链激酶会导致循环血液中纤溶酶激活和出血倾向增加。预先静脉输注FOY和t-AMCHA可抑制此类反应。从上述结果可以得出结论,FOY对激肽形成和纤溶活性有抑制作用。

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