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依布硒啉对牛和大鼠一氧化氮合酶活性的影响会被硫醇改变。

Effect of ebselen on bovine and rat nitric oxide synthase activity is modified by thiols.

作者信息

Hattori R, Yui Y, Shinoda E, Inoue R, Aoyama T, Masayasu H, Kawai C, Sasayama S

机构信息

Third Division, Department of Internal Medicine, Faculty of Medicine, Kyoto University, Japan.

出版信息

Jpn J Pharmacol. 1996 Oct;72(2):191-3. doi: 10.1254/jjp.72.191.

Abstract

The inhibition of nitric oxide synthase (NOS) by ebselen, 2-phenyl-1,2-benzisoselenazole-3(2H)-one, was reversed by the addition of 10(-5) M dithiothreitol, suggesting that ebselen reacts with a critical thiol group of NOS in the inhibitory mechanism. In the presence of 10(-4) to 10(-3)M dithiothreitol, ebselen dose-dependently enhanced NOS activity, implicating another interaction of ebselen with NOS under these conditions. Thus, the effect of ebselen on the NOS activity is modified by thiols.

摘要

依布硒啉(2-苯基-1,2-苯并异硒唑-3(2H)-酮)对一氧化氮合酶(NOS)的抑制作用可通过添加10⁻⁵M二硫苏糖醇而逆转,这表明依布硒啉在抑制机制中与NOS的一个关键巯基发生反应。在存在10⁻⁴至10⁻³M二硫苏糖醇的情况下,依布硒啉剂量依赖性地增强NOS活性,这意味着在这些条件下依布硒啉与NOS存在另一种相互作用。因此,巯基可改变依布硒啉对NOS活性的影响。

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