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@inbook{1482480, author = {Řemínek, Roman and Glatz, Zdeněk and Thormann, Wolfgang}, address = {USA}, booktitle = {Targeting Enzymes for Pharmaceutical Development: Methods and Protocols}, doi = {http://dx.doi.org/10.1007/978-1-0716-0163-1_11}, edition = {1.}, editor = {N.E. Labrou}, keywords = {Capillary electrophoresis; Enantioselective separation; Cytochrome P450; CYP3A4; Ketamine}, howpublished = {tištěná verze "print"}, language = {eng}, location = {USA}, isbn = {978-1-0716-0162-4}, pages = {167-178}, publisher = {Springer}, title = {Online Enantioselective Capillary Electrophoretic Method for Screening Cytochrome P450 3A4 Inhibitors}, url = {https://link.springer.com/protocol/10.1007%2F978-1-0716-0163-1_11}, year = {2020} }
TY - CHAP ID - 1482480 AU - Řemínek, Roman - Glatz, Zdeněk - Thormann, Wolfgang PY - 2020 TI - Online Enantioselective Capillary Electrophoretic Method for Screening Cytochrome P450 3A4 Inhibitors VL - Targeting Enzymes for Pharmaceutical Development PB - Springer CY - USA SN - 9781071601624 KW - Capillary electrophoresis KW - Enantioselective separation KW - Cytochrome P450 KW - CYP3A4 KW - Ketamine UR - https://link.springer.com/protocol/10.1007%2F978-1-0716-0163-1_11 N2 - The market share of single-enantiomer drugs is steadily increasing. The pharmacodynamics and pharmacokinetics of individual enantiomers can differ considerably. Thus, their characteristics have to be addressed as early as possible in the development process of new pharmaceuticals. Capillary electrophoresis is a promising technique for enantioselective drug metabolism studies due to highly effective separations, minuscule consumption of sample and reagents, compatibility with a variety of detection techniques, high-throughput via automation, and the implementation of on-line procedures. An on-line method comprised of the diffusion-based mixing of cytochrome P450 3A4 with racemic ketamine, incubation of the enzyme reaction, separation of the reaction products S- and R-norketamine and their quantification is presented in this chapter. Since diffusion is an inherent property of all molecules, the method enables the addition of virtually any compound to the reaction mixture without the need for additional optimization of the mixing conditions, and thus can be favorably used for the rapid screening of putative cytochrome P450 3A4 inhibitors. ER -
ŘEMÍNEK, Roman, Zdeněk GLATZ a Wolfgang THORMANN. Online Enantioselective Capillary Electrophoretic Method for Screening Cytochrome P450 3A4 Inhibitors. In N.E. Labrou. \textit{Targeting Enzymes for Pharmaceutical Development: Methods and Protocols}. 1. vyd. USA: Springer, 2020, s.~167-178. Targeting Enzymes for Pharmaceutical Development. ISBN~978-1-0716-0162-4. Dostupné z: https://dx.doi.org/10.1007/978-1-0716-0163-1\_{}11.
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