Binding of ethacrynic acid to hepatic glutathione S-transferases in vivo in the rat.
Binding of ethacrynic acid to hepatic glutathione S-transferases in vivo in the rat.
复制标题
大鼠体内依他尼酸与肝谷胱甘肽 S-转移酶的结合。
DOI：
10.1016/0006-2952(80)90420-7
复制
发表时间：
1980
影响因子：
5.8
通讯作者：
Neil Kaplowitz
中科院分区：
文献类型：
--
作者：
Tadataka Yamada;Neil Kaplowitz
乙炔酸是体外大鼠谷胱甘肽S转移酶的底物(1，2)。在他们确定谷胱甘肽S转移酶在肝脏代谢和乙氰酸的胆汁排泄中的重要性的研究中，Wallin等人(3)建议给药的一小部分但一致的部分选择性和共价结合到转移酶上。这种关联将代表药物与代谢酶的共价结合的独特例子，而不需要事先激活微粒体酶。因此，我们进行了这些研究，以表征乙丙烯酸与谷胱甘肽S转移酶的结合，并描述这种结合的选择性。
Ethacrynic acid is a substrate for rat glutathione S-transferases in vitro (1, 2). In their study defining the importance of the glutathione S-transferases in the hepatic metabolism and biliary excretion of ethacrynic acid, Wallin et al.(3) suggested that a small but consistent portion of the administered drug was bound selectively and covalently to the transferases. Such an association would represent a unique example of covalent binding of a drug to the metabolizing enzyme without prior microsomal enzyme activation. We have undertaken these studies, therefore, to characterize the binding of ethacrynic acid to the glutathione S-transferases and to delineate the selectivity of this binding.