STUDIES WITH ALKYLATING ESTERS .I. FATE OF ETHYLENE DIMETHANESULPHONATE

The fate of 14C- and 35S-ethylene dimethanesulphonate (EDS) has been studied in the mouse, rat, rabbit and monkey and compared with that of Myleran, a homologue of EDS. The rat and mouse excreted mainly unchanged 35S-EDS, whereas from the rabbit and monkey only a minor proportion of the unhydrolysed ester was recovered in the urine. Methane sulphonic acid was the only radioactive urinary metabolite, and in this respect no species variation was encountered. In the rat 1,2-14C-EDS gave no evidence of simple hydrolysis since ethylene glycol was not found as a urinary metabolite. Expired radioactive carbon dioxide accounted for 5-8 per cent of the dose. Tissue distribution studies in the mouse show bone, blood and spleen have some selective uptake of EDS; the compound is only slowly cleared from these tissues. The relevance of the findings are discussed and related to comparable studies with Myleran in relation to the biological activity of both compounds. © 1969.