Distribution of 14C labeled at dioxopiperazine or methyl morpholine group of probimane by whole body autoradiography

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.