McGlinchey G, Coakley C B, Gestautus-Tansey V, Gault J, Spillane W J
J Pharm Sci. 1982 Jun;71(6):661-5. doi: 10.1002/jps.2600710614.
The sweet compounds 2-methyl- and 3-methylcyclohexyl- and 2-cyclohexenylsulfamates were fed to Wistar albino rats. The urine (and feces in the case of 2-cyclohexenylsulfamate) was examined for possible amine, ketone, and alcohol metabolites. The total percent of metabolites formed was low and the hexenyl compound gave a particularly small quantity of metabolite. The results with these compounds are compared with those obtained from earlier in vivo studies with cyclamate and other sulfamates. In complementary in vitro studies, the four sweetest sulfamates, namely, cyclamate, cycloheptyl-, cyclooctyl-, and cyclopentylsulfamates were incubated with the cell-free extract of bacteria isolated from the feces of cyclamate fed rats. Some correlation was apparent between these in vitro experiments and previous in vivo studies. Preliminary mutagenicity testing (the Ames test) of some amines (corresponding to the sulfamates studied) has been carried out.
将甜味化合物2-甲基环己基氨基磺酸酯、3-甲基环己基氨基磺酸酯和2-环己烯基氨基磺酸酯喂给Wistar白化大鼠。检测尿液（对于2-环己烯基氨基磺酸酯还检测粪便）中是否存在可能的胺、酮和醇类代谢产物。形成的代谢产物的总百分比很低，且己烯基化合物产生的代谢产物量特别少。将这些化合物的结果与早期用环己基氨基磺酸酯和其他氨基磺酸酯进行的体内研究结果进行比较。在补充性的体外研究中，将四种最甜的氨基磺酸酯，即环己基氨基磺酸酯、环庚基氨基磺酸酯、环辛基氨基磺酸酯和环戊基氨基磺酸酯与从喂食环己基氨基磺酸酯的大鼠粪便中分离出的细菌的无细胞提取物一起孵育。这些体外实验与先前的体内研究之间存在明显的相关性。已经对一些胺（对应于所研究的氨基磺酸酯）进行了初步的致突变性测试（艾姆斯试验）。
