Lu D Y, Xu B, Zhang X, Chen R T
Shanghai Institute of Materia Medica, Chinese Academy of Sciences.
Zhongguo Yao Li Xue Bao. 1993 Mar;14(2):171-3.
Probimane (AT-2153) is a new anticancer compound. It was first developed in this Institute. It is effective against mouse tumors S37, S180, Lewis lung carcinoma, L1210 and human pulmonary adenocarcinoma heterotransplanted into nude mice. In the present work, 14C was labeled at central dioxopiperazine or methyl morpholine group of probimane 120 mg.kg-1 was injected iv in mice bearing Lewis lung carcinoma by whole body autoradiography. The results showed that probimane was broken into at least two parts: a central part and a methyl morpholine group. The central part of compound hardly penetrated through the blood-brain barrier, but accumulated in the urinary bladder. The methyl morpholine group showed a high affinity to tumor tissue and accumulated in spleen, bone and liver.
丙亚胺（AT - 2153）是一种新型抗癌化合物。它最初是由本研究所研制的。它对小鼠肿瘤S37、S180、Lewis肺癌、L1210以及移植到裸鼠体内的人肺腺癌有效。在本研究中，用14C标记丙亚胺120毫克·千克-1，通过全身放射自显影术静脉注射到患有Lewis肺癌的小鼠体内。结果表明，丙亚胺分解为至少两部分：中心部分和甲基吗啉基团。化合物的中心部分几乎不能穿透血脑屏障，但在膀胱中积累。甲基吗啉基团对肿瘤组织表现出高亲和力，并在脾脏、骨骼和肝脏中积累。
