Literature DB >> 14743969

Hepatic metabolism of the new antipsychotic agent, mazapertine, in rat--API-MS/MS identification of metabolites.

W N Wu1, L A McKown, A B Reitz.   

Abstract

The In vitro biotransformation of the antipsychotic agent, mazapertine was studied after incubation with rat hepatic S9 fraction in the presence of an NADPH-generating system. Unchanged mazapertine (42% of the sample) plus 12 metabolites were profiled, quantified, and tentatively identified on the basis of API (ionspray)-MS/MS data. The proposed metabolic pathways for mazapertine are proposed, and the 6 metabolic pathways are: (1) phenylhydroxylation, (2) piperidyl oxidation, (3) O-dealkylation, (4) N-dephenylation, (5) oxidative N-debenzylation, and (6) dehydration. Pathways 1 to 3 formed 4-OH-phenyl (M1, 10%) and 4-OH-piperidyl (M2, 9%)-mazapertine, O-desisopropyl mazapertine (M3, 17%), and N-desbenzoylpiperidine-mazapertine (M8, 14%) as 4 major metabolites. Mazapertine is extensively metabolized in rat hepatic S9 fraction.

Entities:  

Mesh：

Substances：

Year:  2003        PMID： 14743969     DOI： 10.1007/BF03220180

Source DB:  PubMed          Journal:  Eur J Drug Metab Pharmacokinet        ISSN： 0378-7966            Impact factor:   2.441


  3 in total

1.  A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.

Authors:  A B Reitz; D J Bennett; P S Blum; E E Codd; C A Maryanoff; M E Ortegon; M J Renzi; M K Scott; R P Shank; J L Vaught
Journal:  J Med Chem       Date:  1994-04-15       Impact factor: 7.446

2.  In vitro biotransformation of the new antipsychotic agent, RWJ-46344 in rat hepatic S9 fraction: API-MS/MS/MS identification of metabolites.

Authors:  W N Wu; L A McKown; M D Moyer; A B Reitz
Journal:  J Pharm Biomed Anal       Date:  2000-12-15       Impact factor: 3.935

3.  Biotransformation of the antipsychotic agent, mazapertine, in dog--mass spectral characterization and identification of metabolites.

Authors:  W N Wu; L A McKown; A R Takacs; W J Jones; A B Reitz
Journal:  Xenobiotica       Date:  1999-05       Impact factor: 1.908
  3 in total
  4 in total

1.  Hepatic metabolism of two alpha-1A-adrenergic receptor antagonists, phthalimide-phenylpiperazine analogs (RWJ-69205 and RWJ-69471), in the rat, dog and human.

Authors:  W N Wu; L A McKown; G H Kuo
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2006 Oct-Dec       Impact factor: 2.441

2.  Metabolism of the new alpha-1A-adrenergic receptor antagonist, phthalimide-phenylpiperazine analog (RWJ-69442), in rat, dog and human hepatic S9 fractions, and in rats.

Authors:  W N Wu; L A McKown; G H Kuo
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2005 Jan-Jun       Impact factor: 2.441

3.  Metabolism of the alpha-1A-adrenergic receptor antagonist, pyridine-phenylpiperazine analog (RWJ-69597), in rat, dog and human hepatic S9 fractions -API-MS/MS identification of metabolites.

Authors:  W N Wu; L A McKown; G H Kuo
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2005 Jan-Jun       Impact factor: 2.441

4.  Metabolic fate of the antipsychotic agent, mazapertine, in man--API-MS and MS/MS identification of urinary metabolites.

Authors:  Wu-Nan Wu; Linda A McKown; Allen B Reitz
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2007 Jul-Sep       Impact factor: 2.441
  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.