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  1. Article ; Online: An improved method for cytochrome p450 reaction phenotyping using a sequential qualitative-then-quantitative approach.

    Doran, Angela C / Dantonio, Alyssa L / Gualtieri, Gabrielle M / Balesano, Amanda / Landers, Connor / Burchett, Woodrow / Goosen, Theunis C / Obach, R Scott

    Drug metabolism and disposition: the biological fate of chemicals

    2022  

    Abstract: Cytochrome P450 reaction phenotyping to determine the fraction of metabolism values ( ... ...

    Abstract Cytochrome P450 reaction phenotyping to determine the fraction of metabolism values (f
    Language English
    Publishing date 2022-07-01
    Publishing country United States
    Document type Journal Article
    ZDB-ID 186795-7
    ISSN 1521-009X ; 0090-9556
    ISSN (online) 1521-009X
    ISSN 0090-9556
    DOI 10.1124/dmd.122.000883
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Defining the Selectivity of Chemical Inhibitors Used for Cytochrome P450 Reaction Phenotyping: Overcoming Selectivity Limitations with a Six-Parameter Inhibition Curve-Fitting Approach.

    Doran, Angela C / Burchett, Woodrow / Landers, Connor / Gualtieri, Gabrielle M / Balesano, Amanda / Eng, Heather / Dantonio, Alyssa L / Goosen, Theunis C / Obach, R Scott

    Drug metabolism and disposition: the biological fate of chemicals

    2022  

    Abstract: The utility of chemical inhibitors in cytochrome P450 (CYP) reaction phenotyping is highly dependent on their selectivity and potency for their target CYP isoforms. In the present study, seventeen inhibitors of CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A4/5 ...

    Abstract The utility of chemical inhibitors in cytochrome P450 (CYP) reaction phenotyping is highly dependent on their selectivity and potency for their target CYP isoforms. In the present study, seventeen inhibitors of CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A4/5 commonly used in reaction phenotyping were evaluated for their cross-enzyme selectivity in pooled human liver microsomes. The data were evaluated using a statistical desirability analysis to identify (1) inhibitors of superior selectivity for reaction phenotyping and (2) optimal concentrations for each. Among the inhibitors evaluated, α-naphthoflavone, furafylline, sulfaphenazole, tienilic acid,
    Language English
    Publishing date 2022-07-01
    Publishing country United States
    Document type Journal Article
    ZDB-ID 186795-7
    ISSN 1521-009X ; 0090-9556
    ISSN (online) 1521-009X
    ISSN 0090-9556
    DOI 10.1124/dmd.122.000884
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

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