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In vitro identification of the human cytochrome p450 enzymes involved in the oxidative metabolism of loxapine
In vitro studies were conducted to identify the hepatic cytochrome P450 (CYP) enzymes responsible for the oxidative metabolism of loxapine to 8‐hydroxyloxapine, 7‐hydroxyloxapine, N‐desmethylloxapineExpand
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Anticonvulsant properties of various acetylhydrazones, oxamoylhydrazones and semicarbazones derived from aromatic and unsaturated carbonyl compounds.
Various acetylhydrazones, oxamoylhydrazones and semicarbazones were prepared as candidate anticonvulsants with a view to examining the viability of a putative binding site hypothesis. Atomic chargeExpand
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Nuclear magnetic resonance spectroscopy as a quantitative tool to determine the concentrations of biologically produced metabolites: implications in metabolites in safety testing.
Nuclear magnetic resonance (NMR) spectroscopy has traditionally been considered as an indispensable tool in elucidating structures of metabolites. With the advent of Fourier transform (FT)Expand
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Formation of the quaternary ammonium-linked glucuronide of nicotine in human liver microsomes: identification and stereoselectivity in the kinetics.
The formation of the N1-glucuronide metabolite of each nicotine enantiomer was studied in pooled human liver microsomes (n = 6). The metabolite formed from natural S(-)-nicotine was identified byExpand
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Proton-Pumping-ATPase-Targeted Antifungal Activity of a Novel Conjugated Styryl Ketone
ABSTRACT NC1175 (3-[3-(4-chlorophenyl)-2-propenoyl]-4-[2-(4-chlorophenyl)vinylene]-1-ethyl-4-piperidinol hydrochloride) is a novel thiol-blocking conjugated styryl ketone that exhibits activityExpand
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Metabolism of Prazosin in Rat, Dog, and Human Liver Microsomes and Cryopreserved Rat and Human Hepatocytes and Characterization of Metabolites by Liquid Chromatography/Tandem Mass Spectrometry
Prazosin (2-[4-(2-furanoyl)-piperazin-1-yl]-4-amino-6,7-dimethoxyquinazoline) is an antihypertensive agent that was introduced to the market in 1976. It has since established an excellent safetyExpand
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Quaternary ammonium-linked glucuronidation of 1-substituted imidazoles: studies of human UDP-glucuronosyltransferases involved and substrate specificities.
A series of eight 1-substituted imidazoles was investigated as model substrates for glucuronidation at an aromatic tertiary amine of polyaza heterocyclic ring systems. The humanExpand
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Quaternary ammonium-linked glucuronidation of 1-substituted imidazoles by liver microsomes: interspecies differences and structure-metabolism relationships.
N-Glucuronidation at an aromatic tertiary amine of 5-membered polyaza ring systems was investigated for a model series of eight 1-substituted imidazoles in liver microsomes from five species. TheExpand
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In-vitro and in-vivo susceptibility of Aspergillus fumigatus to a novel conjugated styryl ketone.
We investigated the in-vitro and in-vivo susceptibility of Aspergillus fumigatus to the novel conjugated styryl ketone NC1175 and the results were compared with those obtained for amphotericin B andExpand
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4-(beta-Arylvinyl)-3-(beta-arylvinylketo)-1-ethyl-4-piperidinols and related compounds: a novel class of cytotoxic and anticancer agents.
The syntheses of a series of 1-aryl-5-diethylamino-1-penten-3-one hydrochlorides 1 and 1-aryl-3-diethylamino-1-propanone hydrochlorides 4 were accomplished. Attempts to prepare the correspondingExpand
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