Hellman B, Andersson B S, Slanina P, Mohammed A, Brandt I, Beran M
Med Oncol Tumor Pharmacother. 1986;3(2):87-94. doi: 10.1007/BF02934559.
The distribution of 14C-labelled m-AMSA was studied in rats and pigmented mice using whole body autoradiography. The agent rapidly disappeared from the blood, accumulating in significant amounts in large parenchymal organs, certain endocrine tissues, and the retina of the pigmented mouse eye. The hemopoietic and lymphoid tissues showed a moderate uptake of radioactivity with the highest concentration observed in the thymus. The autoradiograms indicated a rapid excretion of radioactivity via the liver, kidney and the glandular part of the gastric mucosa. The distribution pattern of label from 14C-m-AMSA remained unaffected by pretreatment of animals with high dose (500 mg kg-1 b.w.) of cytosine arabinoside. Injection of unlabelled m-AMSA (7 mg kg-1 b.w.) to growing rats 24 h before sacrifice resulted in a highly significant (P less than 0.001) inhibition of 3H-thymidine incorporation into the DNA of thymus and spleen. A less pronounced reduction was observed in the kidney, adrenal, lung and testes. The thymidine incorporation into the DNA of bone marrow was markedly suppressed when calculated per dry weight, but increased when related to the DNA content, suggesting early regeneration of the remaining cells. In contrast, no significant effects were observed on the DNA synthesis in small intestine and liver.
利用全身放射自显影技术，研究了14C标记的间-苯丙氨酸氮芥（m-AMSA）在大鼠和有色小鼠体内的分布情况。该药物迅速从血液中消失，大量蓄积于大型实质器官、某些内分泌组织以及有色小鼠眼睛的视网膜中。造血和淋巴组织对放射性有适度摄取，其中胸腺中的浓度最高。放射自显影片显示放射性通过肝脏、肾脏和胃黏膜的腺体部分迅速排泄。用高剂量（500毫克/千克体重）的阿糖胞苷预处理动物后，14C-m-AMSA标记的分布模式未受影响。在处死前24小时给生长中的大鼠注射未标记的m-AMSA（7毫克/千克体重），导致胸腺和脾脏DNA中3H-胸腺嘧啶核苷掺入量受到高度显著抑制（P小于0.001）。在肾脏、肾上腺、肺和睾丸中观察到的抑制作用较弱。按干重计算，骨髓DNA中的胸腺嘧啶核苷掺入量明显受到抑制，但与DNA含量相关时则增加，这表明剩余细胞早期再生。相比之下，小肠和肝脏中的DNA合成未观察到显著影响。
