Deoxyfructosylserotonin (DFS) has been shown in in vitro tests to inhibit L-DOPA-oxidase and also to suppress the multiplication of Mycobacterium leprae. The possible therapeutic use of DFS makes necessary the study of its metabolic fate in animal models. Labelled [14C]-DFS was synthesized by condensation of serotonin and [14C]-glucose and administered per os or intravenously to rats and mice. After oral administration, some of the radioactivity transited through the intestinal tract to be excreted in feces (20-60% of the dose) and some was destroyed in the pH conditions of the intestine and further metabolized by the flora, producing 14CO2 in the expired air (10-40% of the dose). Radioactivity excreted in the urine amounted to 8-15% after 24 h. After intravenous administration, 60-90% of the dose had already been excreted in the urine after 8 h. Feces and CO2 accounted for 5-10% each. In the urine, for both routes of administration, beside DFS, half of the radioactivity corresponded to the glucuronide conjugate, while in the feces all the radioactivity found was unchanged DFS. Whole animal body autoradiography showed the presence of radioactivity in all the organs (1-2% of the dose) mainly resulting from the incorporation of labelled carbon from glucose and CO2. These results, obtained in healthy rats, demonstrate poor intestinal absorption of DFS (10% of the dose) and when it is absorbed, rapid urinary excretion. For its possible therapeutic use as an anti-leprosy drug in humans, derivatives with higher bioavailability must be attained.