Abstract
Niaprazine (NOPRON®) and major urinary metabolites were identified in rat, dog and man by mass spectrometry after a single oral dose of the drug. Metabolism of niaprazine occurred by N-dealkylation, N-dearylation, aromatic hydroxylation and N-oxidation. EI and DCI-NH 3 mass spectra allowed the structures of most metabolites to be established. Hydroxylation of niaprazine was proved by formation of BSTFA derivatives. Both aliphatic and aromatic N-oxidation occurred. Aliphatic N-oxides, reduced by SO 2, gave mass spectra characterized by the ions M-16, M-18 and Cope rearrangement; aromatic N-oxides, reduced by TiCl 3 and not by SO 2, gave the ions M-16 and M-17.
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