Hepatic Metabolism of the New Antipsychotic Agent, Mazapertine, in Rat - API-MS/MS Identification of Metabolites

European Journal of Drug Metabolism and Pharmacokinetics

Volumn 28, Issue 4, 2003, Pages 279-286

  Wu, W N ^a,b   McKown, L A ^a   Reitz, A B ^a  

^a J W Johnson Pharmaceutical Res I   (United States)

^b LLC   (United States)

Author keywords

Antipsychotic agent; In vitro metabolism; Mazapertine; Ms ms; Rat hepatic S9

Indexed keywords

4 HYDROXYPHENYLMAZAPERTINE; 4 HYDROXYPIPERIDYLMAZAPERTINE; DRUG METABOLITE; MAZAPERTINE; N DESBENZOYLPIPERIDINE MAZAPERTINE; NEUROLEPTIC AGENT; NITROGEN; O DESISOPROPYL MAZAPERTINE; OXYGEN; PHENYL GROUP; PIPERIDINE DERIVATIVE; REDUCED NICOTINAMIDE ADENINE DINUCLEOTIDE PHOSPHATE; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DEALKYLATION; DEHYDRATION; DRUG METABOLISM; DRUG TRANSFORMATION; HYDROXYLATION; INCUBATION TIME; LIVER METABOLISM; MASS SPECTROMETRY; METABOLISM; METABOLITE; NONHUMAN; OXIDATION;

EID: 0347915717     PISSN: 03787966     EISSN: None     Source Type: Journal    
DOI: 10.1007/BF03220180     Document Type: Article

References (12)

1. Buclin, T., Stucki, R., Jaquet-Mueller, F., Munafo, A., Bauldauf, C., Brunner-Ferber, F., and Biollaz, J., (1993): Tolerability and psychopharmacological profile of the novel antipsychotic mazapertine (RWJ-37796) in healthy volunteers. Clinical Pharmacology and Therapeutics, 53, 179 (abstract, 94th Annual Meeting of the American Society for Clinical Pharmacology and Therapeutics).
2. Buclin, T., Stucki, R., Jaquet-Mueller, F., Munafo, A., Bauldauf, C., Brunner-Ferber, F., Piquet, V., and Biollaz, J., (1993): Tolerance, psychopharmacological profile and pharmacokinetics of a new neuroleptic, mazapertine (RWJ-37796), in healthy volunteers, Schweizerische Medizinische Wochenschrift, 123 (16, S50), 39
3. 1A-adrenergic affinity and a low potential for extrapyramidal effects. J. Med. Chem., 37, 1060-1062.
4. Reitz, A.B., McDonnell, M.E., Baxter, E.W., Codd, E.E., and Wu, W.N., (1997): The synthesis and evaluation of the major metabolites of mazapertine, Bioorganic & Medicinal Chemistry Letters, 7, 1927-1930.
5. Wu, W.N., McKown, L.A., Gauthier, A.D., Jones, W.J., and Takacs, A.R., (1994): Metabolism and excretion of the antipsychotic agent, RWJ-37796 in rats. Pharm. Res. 11, S-336 (abstract, the 9th AAPS Annual Meeting).
6. Wu, W.N., McKown, L.A., Jones, W.J. Takacs, A.R., Reitz, A.B., and McDonnell, M.E., (1994): Mass spectral characterization and identification of the metabolites of the antipsychotic agent. RWJ-37796, in dogs, Proceedings of the 42nd ASMS Conference on Mass Spectrometry, 344.
7. tm Supplement, 1, PS36 (abstract, the 13th AAPS Annual Meeting).
8. Gisclon, L.G., and Curtin, C.R., (1993): The effect of food on the bioavailability (BA) of a new antipsychotic drug (RWJ-37796), Pharm. Res., 10, S-398 (abstract, the 8th AAPS Annual Meeting).
9. Wu, W.N., Gisclon, L.G., and McKown, L.A., (1995): Metabolism of the antipsychotic agent, mazapertine succinate: structural elucidation of human urinary metabolites of mazapertine using ic/ionspray-ms/ms. Proceedings of the 43rd ASMS Conference on Mass Spectrometry and Allied Topics, 56.
10. Wu, W.N., McKown, L.A., Takacs, A.R., and Reitz, A.B., (1997): In vitro metabolism of the new antipsychotic agent, RWJ-46344-002, in rat hepatic S9 fraction. ISSX Proceedings, 161 (abstract, the 6th European ISSX Meeting).
11. Wu, W.N., McKown, L.A., Moyer, M.D., and Reitz, A.B., (2000): In vitro biotransformation of the new antipsychotic agent, RWJ-46344 in rat hepatic S9 fraction: api-ms/ms identifcation of metabolites, J. Pharm. Biomed. Anal. 24, 307-316.
12. Wu, W.N., Mckown, L.A., Takacs, A.R., Jones, W.J., and Reitz, A.B., (1999): Biotransformation of the antipsychotic agent, mazapertine, in dog, Xenobiotica, 29, 453-466.