Identification of urinary metabolites of ecabapide in rat

Article abstract of DOI:10.3109/00498259509061869

¹⁴C-Ecabapide, 3-[[[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl]methyl]amino-N-methyl[¹⁴ C]benzamide, was dosed orally to rat (100 mg/kg). Within 48 h after dosing, 36.7 ± 5.4 and 55.7 ± 11.8% of the administered radioactivity was recovered from urine and faeces respectively. The unchanged drug was the major compound excreted in the urine and accounted for 37% of the urinary radioactivity. Seven urinary metabolites were purified by preparative hplc and their structures were elucidated by mass and ¹H-nmr spectrometry. The major metabolic pathway of ecabapide was found to be the formation of 3-amino-N-methylbenzamide produced by N-dealkylation of the secondary amine at the 3-position of the benzamide moiety followed by acetylation. Further metabolic pathways of the N-methylbenzamide moiety were N-demethylation via the carbinolamine derivatives, and/or aromatic hydroxylation followed by glucuronidation.

Full text of DOI:10.3109/00498259509061869

Xenobiotica
the fate of foreign compounds in biological systems
ISSN: 0049-8254 (Print) 1366-5928 (Online) Journal homepage: http://www.tandfonline.com/loi/ixen20
Identification of urinary metabolites of ecabapide
in rat
Y. Fujimaki, T. Hosokami & K. Ono
To cite this article: Y. Fujimaki, T. Hosokami & K. Ono (1995) Identification of urinary
metabolites of ecabapide in rat, Xenobiotica, 25:5, 501-510
To link to this article: http://dx.doi.org/10.3109/00498259509061869
Published online: 27 Aug 2009.
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Date: 07 November 2015, At: 08:14