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Characterization of the human hepatic cytochromes P450 involved in the in vitro oxidation of clozapine.
It was aimed to identify the cytochrome(s) P450 (CYPs) involved in the N-demethylation and N-oxidation of clozapine (CLZ) by various approaches using human liver microsomes or microsomes from humanExpand
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In vitro characterization of the metabolism of haloperidol using recombinant cytochrome p450 enzymes and human liver microsomes.
A systematic in vitro study was carried out to elucidate the enzymes responsible for the metabolism of haloperidol (HAL) using human liver microsomes and recombinant human cytochrome P450 isoenzymes.Expand
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Stability and enzymatic hydrolysis of quaternary ammonium-linked glucuronide metabolites of drugs with an aliphatic tertiary amine-implications for analysis.
Quaternary ammonium-linked glucuronide (N+-glucuronide) metabolites formed at aliphatic tertiary amine functional groups of xenobiotics have not been previously systematically studied with respect toExpand
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N-oxygenation of clozapine by flavin-containing monooxygenase.
The involvement of FMO in the N-oxygenation of CLZ was investigated by use of purified FMOs and human liver microsomes that contained the mean amount of immunoreactive FMO3 relative to other humanExpand
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Characterization of metabolites of clozapine N-oxide in the rat by micro-column high performance liquid chromatography/mass spectrometry with electrospray interface.
The metabolism of clozapine N-oxide was investigated in the rat (n = 6) after a single oral dose of 20 mg kg-1. The organic extracts of rat urine were separated by conventional high performanceExpand
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N(+)-glucuronidation of aliphatic tertiary amines in human: antidepressant versus antipsychotic drugs.
1. Metabolic N(+)-glucuronidation of aliphatic tertiary amine antidepressant or antipsychotic drugs was investigated in man. In each case, urine was collected either from patients and/or from healthyExpand
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Metabolism of phenothiazine and butyrophenone antipsychotic drugs. A review of some recent research findings and clinical implications.
Whereas some metabolites of antipsychotic drugs are psychoactive and contribute to clinical improvement, recent studies have provided evidence that certain metabolites contribute to side-effectsExpand
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Identification of phase-I and phase-II metabolites of fluphenazine in rat bile. Intact glucuronide and sulfate conjugates.
In rat bile following ip administration of fluphenazine (FLU) dihydrochloride (20 mg/kg body weight), phase-I metabolites 7-hydroxyfluphenazine (7-HOFLU) and FLU sulfoxide (FLUSO), together withExpand
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Synthesis and characterization of quaternary ammonium-linked glucuronide metabolites of drugs with an aliphatic tertiary amine group.
A synthetic approach was developed to make the quaternary ammonium-linked glucuronide metabolites of compounds with an aliphatic tertiary amine group. The key step involved quaternization of theExpand
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Intersubject Variation in the Pharmacokinetics of Haloperidol and Reduced Haloperidol
Single oral doses (5 mg) of haloperidol were administered to 36 healthy men (26 black, 10 white) of whom 28 (22 black, 6 white) completed the study. Plasma samples harvested over 96 hours wereExpand
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