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Activation and Detoxification of N-2-Fluorenylacetamide in Man^*

( Carcinogenesis Studies Branch and Clinical Pharmacology and Experimental Therapeutics Service, Medicine Branch, National Cancer Institute, Bethesda, Maryland

Five patients with various malignant diseases excreted rapidly, chiefly in the urine, isotope from a single oral tracer dose of N-2-fluorenyl-9-C¹⁴-acetamide. The urine contained 24–30 per cent of the dose of the detoxification product, N-(7-hydroxy-2-fluorenyl)acetamide, as the glucuronic acid conjugate. The other major metabolite was N-hydroxy-2-fluorenylacetamide, a proximate carcinogen derived from the compound administered. The amount of this compound varied from 4.4 to 13 per cent of the dose.

^* An abstract of this work has appeared (Proc. Am. Assoc. Cancer Res.) 4:70, 1963).

Received 10/ 1/63.

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