Baumeister M
Toxicol Lett. 1982 Aug;12(4):281-8. doi: 10.1016/0378-4274(82)90252-1.
The secondary and tertiary amines morpholine, aminopyrine and cimetidine as well as their nitroso products were examined for mutagenicity with the Ames Salmonella typhimurium microsome test (strains TA1535 and TA100) and the host-mediated assay. The formation of mutagenic nitroso compounds from morpholine and aminopyrine in the presence of nitrite could be demonstrated in artificial gastric juice and was confirmed in the stomach of mice in vivo. In contrast, the positive response of the chemical nitrosation in vitro with cimetidine did not match with the mammalian host-mediated assay results. To enhance sensitivity the role of modifiers of nitrosation, such as ascorbic acid and thiocyanate as well as the influence of biotransformation were studied.
利用鼠伤寒沙门氏菌微粒体试验(TA1535和TA100菌株)和宿主介导试验,检测了仲胺和叔胺吗啡啉、氨基比林和西咪替丁及其亚硝基产物的致突变性。在人工胃液中可证明在亚硝酸盐存在下由吗啡啉和氨基比林形成诱变亚硝基化合物,并且在小鼠胃内体内得到证实。相比之下,西咪替丁体外化学亚硝化的阳性反应与哺乳动物宿主介导试验结果不相符。为提高灵敏度,研究了亚硝化修饰剂如抗坏血酸和硫氰酸盐的作用以及生物转化的影响。