Brandt I, Mohammed A, Slanina P
Toxicology. 1981;21(4):317-22. doi: 10.1016/0300-483x(81)90146-3.
Whole body autoradiograms of mice injected with 2,2',3,3',6-[14C]pentachlorobiphenyl (I), 2,3,3',4',6-[14C]pentachlorobiphenyl (II), 2,2',3,5',6-[14C]pentachlorobiphenyl (III) and 2,3',4,5,5'-[14C]pentachlorobiphenyl (IV) showed a specific accumulation of I-III in the lung parenchyma, whereas IV did not accumulate in the lung tissue. The results suggest that chlorobiphenyls with chlorine atoms in the positions 2,3,6 possess a specific affinity for the lung parenchyma. These chlorobiphenyls differ in chemical structure from those which are accumulated in the bronchial mucosa and those which are not taken up in the respiratory tract. The importance of in vivo metabolism in the determination of structure activity relationships is stressed.
给小鼠注射2,2',3,3',6-[¹⁴C]五氯联苯(I)、2,3,3',4',6-[¹⁴C]五氯联苯(II)、2,2',3,5',6-[¹⁴C]五氯联苯(III)和2,3',4,5,5'-[¹⁴C]五氯联苯(IV)后的全身放射自显影片显示,I - III在肺实质中有特异性蓄积,而IV在肺组织中不蓄积。结果表明,在2、3、6位带有氯原子的氯联苯对肺实质具有特异性亲和力。这些氯联苯在化学结构上与那些蓄积在支气管黏膜中的以及那些不被呼吸道摄取的氯联苯不同。强调了体内代谢在确定构效关系中的重要性。