RT Journal Article
SR Electronic
T1 Disposition and metabolism of 3-(3-chlorophenoxy)-N-methylpyrrolidine [14C]-carboxamide in the rat, dog, and man.
JF Drug Metabolism and Disposition
JO Drug Metab Dispos
FD American Society for Pharmacology and Experimental Therapeutics
SP 379
OP 386
VO 4
IS 4
A1 L B Turnbull
A1 L Teng
A1 J Newman
A1 R B Bruce
A1 W R Maynard
YR 1976
UL http://dmd.aspetjournals.org/content/4/4/379.abstract
AB Studies with a 14C-labeled sample have shown that the title compound A is readily absorbed and very rapidly excreted by the rat, dog, and man. The metabolites result from aromatic ring hydroxylation, oxidation, and dealkylation of the urea methyl group, and oxidative ring opening of the pyrrolidine ring. Rat metabolites were 3-(3-chloro-4-hydroxyphenoxy)-N-methyl-l-pyrrolidinecarboxamide (C) 3-(3-chloro-4-hydroxyphenoxy)-1-pyrrolidinecarboxamide (D), 3-(3-chlorohydroxyphenoxy)-1-pyrrolidinecarboxamide (E), 3-(3-chlorophenoxy)-4([(methylamino)-carbonyl]amino)butanoic acid (G), 3-(3-chlorophenoxy)-4[(aminocarbonyl)amino]butanoic acid (H). Dog metabolites were C, D, G, and H. Human metabolites were 3-(3-chloro-4-hydroxyphenoxy)-N-formyl-l-pyrrolidinecarboxamide (F), C, D, G, and H. An electron-capture gas chromatographic assay for the parent compound is described. Whole-body autoradiograms of rat slices and the tissue residue data from these slices are reported and indicate rapid tissue depletion of radioactivity.