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Involvement of CYP3A4 in the metabolism of bromperidol in vitro.
Pharmacol Toxicol. 2000 Mar; 86(3):145-8.PT

Abstract

In this study, human cytochrome P450 isoenzymes (CYP1A2, CYP2C19, CYP2D6, and CYP3A4) expressed in a cell line were used to elucidate their roles in the metabolism of bromperidol. We found that CYP3A4 catalyzes the N-dealkylation of bromperidol and its metabolite, reduced bromperidol. CYP3A4 also catalyzes the dehydration of bromperidol to bromperidol 1,2,3,6-tetrahydropyridine, metabolizes bromperidol to bromperidol pyridinium, and catalyzes the oxidation of reduced bromperidol back to bromperidol. CYP1A2, CYP2C19, and CYP2D6 do not catalyze these reactions.

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Authors+Show Affiliations

Sato S
Department of Psychiatry, Niigata University School of Medicine, Japan.
Someya T
No affiliation info available
Shioiri O
No affiliation info available
Koitabashi T
No affiliation info available
Inoue Y
No affiliation info available

MeSH

Aryl Hydrocarbon HydroxylasesCell FractionationCell LineChromatography, High Pressure LiquidCytochrome P-450 CYP1A2Cytochrome P-450 CYP2C19Cytochrome P-450 CYP2D6Cytochrome P-450 CYP3ACytochrome P-450 Enzyme SystemHaloperidolHumansMicrosomesMixed Function Oxygenases

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

10752674

Citation

Sato, S, et al. "Involvement of CYP3A4 in the Metabolism of Bromperidol in Vitro." Pharmacology & Toxicology, vol. 86, no. 3, 2000, pp. 145-8.
Sato S, Someya T, Shioiri O, et al. Involvement of CYP3A4 in the metabolism of bromperidol in vitro. Pharmacol Toxicol. 2000;86(3):145-8.
Sato, S., Someya, T., Shioiri, O., Koitabashi, T., & Inoue, Y. (2000). Involvement of CYP3A4 in the metabolism of bromperidol in vitro. Pharmacology & Toxicology, 86(3), 145-8.
Sato S, et al. Involvement of CYP3A4 in the Metabolism of Bromperidol in Vitro. Pharmacol Toxicol. 2000;86(3):145-8. PubMed PMID: 10752674.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Involvement of CYP3A4 in the metabolism of bromperidol in vitro. AU - Sato,S, AU - Someya,T, AU - Shioiri,O, AU - Koitabashi,T, AU - Inoue,Y, PY - 2001/2/7/pubmed PY - 2001/2/7/medline PY - 2001/2/7/entrez SP - 145 EP - 8 JF - Pharmacology & toxicology JO - Pharmacol Toxicol VL - 86 IS - 3 N2 - In this study, human cytochrome P450 isoenzymes (CYP1A2, CYP2C19, CYP2D6, and CYP3A4) expressed in a cell line were used to elucidate their roles in the metabolism of bromperidol. We found that CYP3A4 catalyzes the N-dealkylation of bromperidol and its metabolite, reduced bromperidol. CYP3A4 also catalyzes the dehydration of bromperidol to bromperidol 1,2,3,6-tetrahydropyridine, metabolizes bromperidol to bromperidol pyridinium, and catalyzes the oxidation of reduced bromperidol back to bromperidol. CYP1A2, CYP2C19, and CYP2D6 do not catalyze these reactions. SN - 0901-9928 UR - https://www.unboundmedicine.com/medline/citation/10752674/Involvement_of_CYP3A4_in_the_metabolism_of_bromperidol_in_vitro_ L2 - http://ovidsp.ovid.com/ovidweb.cgi?T=JS&PAGE=linkout&SEARCH=10752674.ui DB - PRIME DP - Unbound Medicine ER -
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