Brandt I, Mohammed A, Lydén A, Slanina P
Acta Pharmacol Toxicol (Copenh). 1984 May;54(5):352-60. doi: 10.1111/j.1600-0773.1984.tb01942.x.
The distribution of methylsulphonylpentachloro-[14C]benzene (I), methylthiopentachloro-[14C]benzene (II), 1,4-bis(methylthio)tetrachloro-[14C]benzene (III) and 1,2,4-tris(methylthio)trichloro[14C]benzene (IV) was studied after intravenous injection in mice. The administration of I resulted in a rapid and selective accumulation of radioactivity in the gray matter of the brain, the lung and the zona reticularis of the adrenal cortex. In mice pretreated with metyrapone, or with high dose of unlabelled I, the radioactivity in the tissues was increased, whereas pretreatment with diethyl maleate did not change the disposition of I. In mice injected with II-IV no site of selective accumulation in the tissues was observed. Similarly to I, compounds II-IV were rapidly excreted in bile/faeces and urine. It is proposed that the sulphone group is essential for the high affinity of I for the brain, lung and adrenal cortex.
在给小鼠静脉注射后，研究了甲基磺酰基五氯 - [¹⁴C]苯（I）、甲基硫代五氯 - [¹⁴C]苯（II）、1,4 - 双（甲基硫代）四氯 - [¹⁴C]苯（III）和1,2,4 - 三（甲基硫代）三氯 - [¹⁴C]苯（IV）的分布情况。注射I后，放射性迅速且选择性地在脑灰质、肺和肾上腺皮质网状带中积累。在用甲吡酮预处理的小鼠或用高剂量未标记的I预处理的小鼠中，组织中的放射性增加，而用马来酸二乙酯预处理则不会改变I的分布情况。在注射II - IV的小鼠中，未观察到组织中有选择性积累的部位。与I类似，化合物II - IV迅速经胆汁/粪便和尿液排泄。有人提出，砜基对于I与脑、肺和肾上腺皮质的高亲和力至关重要。
