@article {Tocco330, author = {D J Tocco and F A deLuna and A E Duncan and R W Walker and B H Arison and W J Vandenheuvel}, title = {Physiological disposition and metabolism of 2-aminomethyl-4-(1,1-dimethylethyl)-6-iodophenol hydrochloride.}, volume = {7}, number = {5}, pages = {330--334}, year = {1979}, publisher = {American Society for Pharmacology and Experimental Therapeutics}, abstract = {MK-447-(14)C [2-aminomethyl-4-(1,1-dimethylethyl)-6-iodophenol hydrochloride] was well absorbed and metabolized in man, rats, and dogs. Peak plasma levels of radioactivity were observed in these species 1-2 hr after oral administration of 2 mg/kg to rats and dogs and 25 mg to man. At the peak, parent drug represented about 15\% of the radioactivity in human plasma and only approximately 5\% in rat and dog plasma. The half-life of the parent drug in human plasma was approximately 4 h. Human subjects excreted 96\% of the dose, with 76\% in the urine and 20\% in the feces, in 3 days. Rats excreted 80\% of an oral and 82\% of an intravenous 2-mg/kg dose in 72 hr, with 66\% in the urine and 12-16\% in the feces. In dogs given a 2-mg/kg dose intravenously, the recovery of radioactivity in 72 hr was approximately 99\%, with 85\% in the urine and 14\% in the feces. The major metabolite in rat and dog urine, constituting approximately 90\% of the urine radioactivity, was the O-sulfate conjugate of MK-447. In man, this metabolite accounted for 17\% of the radioactivity in the urine. The major metabolite in human urine, constituting approximately 73\% of the urine radioactivity, was tentatively identified as the N-glucuronide of MK-447. Less than 1\% of the radioactivity in the urine of the three species was in intact MK-447.}, issn = {0090-9556}, URL = {https://dmd.aspetjournals.org/content/7/5/330}, eprint = {https://dmd.aspetjournals.org/content/7/5/330.full.pdf}, journal = {Drug Metabolism and Disposition} }