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甲磺酸加贝酯、卡莫司他和抑肽酶对磷脂酶A2的抑制作用。

Inhibition of phospholipase A2 by gabexate mesilate, camostate and aprotinine.

作者信息

Freise J, Magerstedt P, Schmid K

出版信息

Enzyme. 1983;30(3):209-12. doi: 10.1159/000469576.

Abstract

Gabexate mesilate (FOY, ethyl-p-[6-guanidino-hexanoyloxy]-benzoate-methanesulfonate), camostate (N,N-dimethyl-carbamoylmethyl-4-[4-guanidinobenzoyloxy]-phenylacetate), methanesulfonate (FOYPAN) and aprotinine (Trasylol) were tested for possible inhibition of phospholipase A2. Gabexate mesilate at a concentration of 5 x 10(-4) mol/l and camostate at a concentration of 10(-3) mol/l caused a 50% reduction in enzyme activity. There was no inhibition by aprotinine at clinical doses; 40 million KIU/l were necessary to reduce phospholipase A2 activity by 20%.

摘要

对甲磺酸加贝酯(FOY,对-[6-胍基己酰氧基]苯甲酸乙酯甲磺酸盐)、卡莫司他(N,N-二甲基氨基甲酰甲基-4-[4-胍基苯甲酰氧基]苯乙酸酯)、甲磺酸盐(FOYPAN)和抑肽酶(胰蛋白酶抑制剂)进行了抑制磷脂酶A2的可能性测试。浓度为5×10⁻⁴mol/L的甲磺酸加贝酯和浓度为10⁻³mol/L的卡莫司他可使酶活性降低50%。临床剂量的抑肽酶无抑制作用;需要4000万KIU/L才能使磷脂酶A2活性降低20%。

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