IDENTIFICATION OF URINARY METABOLITES OF PYRILAMINE AFTER ORAL-ADMINISTRATION TO MAN

1. The metabolism of pyrilamine, 2-[4-methoxybenzyl-(2-dimethylaminoel hyl) amino] pyridine, was studied in adult male volunteers after a sin gle 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/TM SCI hyl-N-trimethylsilyl-trifluoroacetamidel-trimethyl c hlorosilane). The structure of metabolites were determined based on EI mass spectra and confirmed with those of authentic standards. 3. Conj ugated metabolites identified in the urine were pyrilamine, O-desmethy lpyril amine, and ring hydroxylated derivatives of pyrilamine. O-desme thylpyrilamine was also detected in low abundance as a free form. 4. T hese metabolites observed in human urine were quite different from tho se previously reported in rat.