1988 Volume 3 Issue 1 Pages 25-32
Biotransformation of 3-[p-trans-4-aminomethyl-cyclohexylcarbonyl)phenyl]propionic acid hydrochloride (TEI-5103) was studied in rats and dogs.
1) Three metabolites which were related chemically to TEI-5103 were detected in urine; they were identified on a UV spectrum, Chromatograph and Mass spectrum by direct comparison with authentic compounds as follows: 3-[p-(4-carboxycyclohexylcarbonyl)phenyl]propionic acid (M-1), p-(4-carboxycyclohexylcarbonyl)benzoic acid (M-2), p-(4-carboxycyclohexylhydroxymethyl)benzoic acid (M-3). Metabolite M-3 was detected only in dogs.
2) In rat plasma, the major metabolites were M-2, unchanged drug and M-1; while in dogs, unchanged drug, M-3 and M-1.
3) After oral and intravenous administration, M-2, unchanged drug and M-1 were mainly excreted to the urine in rats while in dogs, M-3, M-2 and unchanged drug were the main metabolites excreted to the urine.
4) M-2 was mainly excreted with bile in rats. In dogs, M-2 and M-1 were a major metabolites excreted to feces after intravenous administration.
