Remmer H, Scheulen M, Kappus H, Bolt H M
Arch Toxicol. 1977 Dec 30;39(1-2):31-9. doi: 10.1007/BF00343273.
When rats were dosed with 14 microgram/kg 3H-isoproterenol, 3H-radioactivity was measurable in the liver until 48 h. This amount was not different in livers of animals which have been pretreated with diethyl maleate. After exhaustive extraction, a significant amount of 3H-radioactivity from isoproterenol could be detected in the proteins of total liver (homogenate), of cytosol and of microsomes. In the cytosol fraction of diethyl maleate pretreated animals twice the amount of isoproterenol-radioactivity was found in the extracted proteins compared to controls. In the microsomal fraction there was no difference between diethyl maleate pretreated and control animals in the amount of radioactivity incorporated into proteins. In all fractions the radioactivity measurable in the extracted proteins declined with a half life time of about 24 h. The in vivo results on covalent binding of isoproterenol are compared to the irreversible protein binding of ethinyloestradiol in vivo. Quantitatively, these in vivo data are compared to the results on irreversible protein binding obtained during incubations of isoproterenol or ethinyloestradiol with rat liver microsomes.
当给大鼠注射14微克/千克的3H-异丙肾上腺素时，在48小时内肝脏中均可检测到3H放射性。在经马来酸二乙酯预处理的动物肝脏中，该放射性量并无差异。经过彻底提取后，在全肝（匀浆）、胞质溶胶和微粒体的蛋白质中均可检测到大量来自异丙肾上腺素的3H放射性。在经马来酸二乙酯预处理的动物的胞质溶胶部分中，与对照组相比，提取的蛋白质中异丙肾上腺素放射性的含量是对照组的两倍。在微粒体部分，经马来酸二乙酯预处理的动物与对照动物在掺入蛋白质中的放射性量上没有差异。在所有部分中，提取的蛋白质中可测量的放射性以约24小时的半衰期下降。将异丙肾上腺素体内共价结合的结果与乙炔雌二醇在体内的不可逆蛋白质结合进行了比较。从数量上看，这些体内数据与异丙肾上腺素或乙炔雌二醇与大鼠肝脏微粒体孵育期间获得的不可逆蛋白质结合结果进行了比较。
