Schuntner C A, Thompson P G
Aust J Biol Sci. 1978 Apr;31(2):141-8. doi: 10.1071/bi9780141.
Amitraz, 1, 5-di(2, 4-dimethylphenyl)-3-methyl-1, 3, 5-triazapenta-1, 4-diene, labelled with 14C in the 2-methyl groups was applied to B. microplus larvae by an immersion technique. The chemical penetrated readily but never appeared in large amounts internally due to rapid cleavage to N-2, 4-dimethylphenyl-N'-methylformamidine. The expected complementary cleavage product 2, 4-dimethylformanilide was not produced in equivalent quantity. However, large amounts of polar metabolite(s) were produced. Small quantities of 2, 4-dimethylaniline and an unidentified non-polar metabolite were also produced. Of the identified chemicals only amitraz and N-2, 4-dimethylphenyl-N'-methylformamidine were toxic to larvae. Piperonyl butoxide applied simultaneously with amitraz had only a slight effect on metabolism but had a three-fold synergistic effect. SKF 525-A similarly applied had a negligible effect on both metabolism and toxicity.
将在2-甲基基团上标记有14C的双甲脒，即1,5-二（2,4-二甲基苯基）-3-甲基-1,3,5-三氮杂戊-1,4-二烯，通过浸泡技术施用于微小牛蜱幼虫。该化学物质很容易渗透进去，但由于迅速裂解为N-2,4-二甲基苯基-N'-甲基甲脒，所以在体内从未大量出现。预期的互补裂解产物2,4-二甲基甲酰苯胺的产量并不相当。然而，产生了大量的极性代谢物。还产生了少量的2,4-二甲基苯胺和一种未鉴定的非极性代谢物。在已鉴定的化学物质中，只有双甲脒和N-2,4-二甲基苯基-N'-甲基甲脒对幼虫有毒。与双甲脒同时施用的胡椒基丁醚对代谢只有轻微影响，但有三倍的协同作用。同样施用的SKF 525-A对代谢和毒性的影响可忽略不计。
