Document Detail

Metabolic fate of the antipsychotic agent, mazapertine, in man--API-MS and MS/MS identification of urinary metabolites.
MedLine Citation:
PMID:  18062409     Owner:  NLM     Status:  MEDLINE    
The in vivo metabolism of the antipsychotic agent mazapertine was studied after oral administration of mazapertine succinate (40 mg/subject) to two healthy volunteers, and urine (0-24 hours) was obtained for metabolite identification using API-ionspray LC/MS and MS/MS analysis. Unchanged mazapertine (12% of the sample) plus 10 metabolites were profiled, quantified, and tentatively identified on the basis of MS data, Glusulase-hydrolysis, and by comparison to synthetic samples. The formation of mazapertine metabolites are via seven metabolic pathways: (1) phenylhydroxylation, (2) piperidyl oxidation, (3) O-dealkylation, (4) N-dephenylation, (5) oxidative N-debenzylation, (6). depiperidylation, and (7) glucuronidation. Pathways 1, 2, 5 and 7 formed 4-OH-phenyl-mazapertine (M1, 18%) and 4-OH-piperidyl (M2, 14%)-mazapertine, carboxybenzoylpiperidine (M8, 10%) and its glucuronide (M9, 14%) as four major metabolites. Six moderate and minor metabolites (M3-M7 & M10; each < or =10%) formed via a combination of pathways 1-6. Mazapertine is extensively metabolized in humans.
Wu-Nan Wu; Linda A McKown; Allen B Reitz
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  European journal of drug metabolism and pharmacokinetics     Volume:  32     ISSN:  0378-7966     ISO Abbreviation:  Eur J Drug Metab Pharmacokinet     Publication Date:    2007 Jul-Sep
Date Detail:
Created Date:  2007-12-07     Completed Date:  2007-12-27     Revised Date:  2011-02-02    
Medline Journal Info:
Nlm Unique ID:  7608491     Medline TA:  Eur J Drug Metab Pharmacokinet     Country:  Switzerland    
Other Details:
Languages:  eng     Pagination:  171-6     Citation Subset:  IM    
Johnson & Johnson Pharmaceutical Research & Development, LLC, Spring House, PA 19477, USA.
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MeSH Terms
Administration, Oral
Antipsychotic Agents / administration & dosage,  metabolism*,  pharmacokinetics,  urine*
Piperazines / administration & dosage,  metabolism*,  pharmacokinetics,  urine*
Spectrometry, Mass, Electrospray Ionization
Reg. No./Substance:
0/Antipsychotic Agents; 0/Piperazines; 134208-18-7/mazapertine succinate

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