大鼠体内N-亚硝基羟乙基-烷基胺磷酸酯的代谢

Metabolism of N-nitroso-hydroxyethyl-alkylamine phosphate esters in the rat.

作者信息

Frank N, Frei E, Wiessler M

机构信息

Institute of Toxicology and Chemotherapy, German Cancer Research Center, Heidelberg, F.R.G.

出版信息

Toxicology. 1989 Jul 3;57(1):59-67. doi: 10.1016/0300-483x(89)90034-6.

DOI:10.1016/0300-483x(89)90034-6

PMID:2546293

Abstract

The metabolism of 1-(N-methyl-N-nitrosamino)-ethylphosphate and 1-(N-ethyl-N-nitrosamino)-ethylphosphate in the rat was investigated. The determination of blood clearance, organ clearance, excretion of parent compounds in the urine and the exhalation of radiolabeled CO2 originating from a nitrosaminophosphate demonstrated a rapid metabolism of the compounds. The high activity of alkaline phosphatase in kidney caused a very rapid degradation of the nitrosamino phosphates in kidney homogenate, whereas the compounds were relatively stable in liver homogenate and serum. We, therefore, suggest a rapid degradation of such nitrosamino conjugates, if they are formed at all, in vivo.

摘要

研究了大鼠体内1-（N-甲基-N-亚硝基氨基）-乙基磷酸酯和1-（N-乙基-N-亚硝基氨基）-乙基磷酸酯的代谢情况。对血清除率、器官清除率、尿中母体化合物的排泄以及源自亚硝基氨基磷酸酯的放射性标记二氧化碳的呼出量的测定表明，这些化合物代谢迅速。肾脏中碱性磷酸酶的高活性导致肾脏匀浆中亚硝基氨基磷酸酯迅速降解，而这些化合物在肝脏匀浆和血清中相对稳定。因此，我们认为，如果此类亚硝基氨基共轭物在体内形成，它们会迅速降解。