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Studies on the Metabolism of 2-Benzoylaminofluorene-9-C¹⁴ and 2-Acetylaminofluorene-9-C¹⁴ in the Rat^{* ,}

( Radiosotope Laboratory, V A Hospital, Minneapolis, the Department of Physiological Chemistry, University of Minnesota Medical School, Minneapolis, Minn., and the Cancer Research Laboratory, University of Florida, Gainesville, Fla.)

1. The metabolism of 2-benzoylaminofluorene-9-C¹⁴ and 2-acetylaminofluorene-9-C¹⁴ was studied in the rat after intramuscular injection. The administered radioactivity was recovered quantitatively from the tissues and excreta.

2. Approximately 90 per cent of the radioactivity of labeled AAF was excreted in 96 hours, while only 20 per cent of the radioactivity of labeled BAF was found in the excreta. Labeled material was excreted in the urine approximately 10 times faster after injection of AAF than after administration of BAF. The data indicate that AAF is more reactive in vivo than is BAF.

3. Fractionation of the urine with ether at various pH indicated that the major portion of the radioactivity was associated with water-soluble compounds which may be conjugation products. Treatment of the urine with hot sulfuric acid decreased the quantities of water-soluble radioactivity, indicating partial hydrolysis.

4. No AF was recovered from the urine after injection of labeled BAF and only a trace after administration of labeled AAF. AF is not, therefore, considered to be a major end product of the metabolism of BAF or AAF. Since no appreciable difference in the recovery of AF after administration of BAF or AAF was found, there appears to be no relationship between the carcinogenicity of derivatives of AF and the excretion of the free amine.

^* This investigation was supported, in part, by contract AT-(40-1) 1403 with the Atomic Energy Commission.

Reviewed in the Veterans Administration and published with the approval of the Chief Medical Director. The statements and conclusions published by the authors are the result of their own study and do not necessarily reflect the opinion or policy of the Veterans Administration.

Received 11/21/52.