Identification of urinary metabolites of pyrilamine after oral administration to man.
1. The metabolism of pyrilamine, 2-[4-methoxybenzyl-(2-dimethylaminoethyl) amino] pyridine, was studied in adult male volunteers after a single oral dose of 50 mg. 2. Solvent extracts of urine obtained with or without enzyme hydrolysis were analysed by gc/ms after derivatization with MSTFA/TMSCI (N-methyl-N-trimethylsilyl-trifluoroacetamide/trimethyl chlorosilane). The structure of metabolites were determined based on EI mass spectra and confirmed with those of authentic standards. 3. Conjugated metabolites identified in the urine were pyrilamine, O-desmethylpyrilamine, and ring hydroxylated derivatives of pyrilamine. O-desmethylpyrilamine was also detected in low abundance as a free form. 4. These metabolites observed in human urine were quite different from those previously reported in rat.
Chung
B C
BC
Doping Control Center, Korea Institute of Science and Technology, Seoul.
Kim
D H
DH
Jung
B H
BH
Eom
K
K
Slikker
W
W
Park
J
J
D000284:Administration, Oral; D000328:Adult; D008401:Gas Chromatography-Mass Spectrometry; D006801:Humans; D008297:Male; D011738:Pyrilamine / Q000008:administration & dosage / Q000378:metabolism / Q000652:urine*
D011738:Pyrilamine