Substituted Imidazole of 5-Fluoro-2-[4-[(2-phenyl-1H-imidazol-5-yl)methyl]-1-piperazinyl]pyrimidine Inactivates Cytochrome P450 2D6 by Protein Adduction

5-Fluoro-2-[4-[(2-phenyl-1H-imidazol-5-yl)methyl]-1-piperazinyl]pyrimidine (SCH 66712) is a potent mechanism-based inactivator of human cytochrome P450 2D6 that displays type I binding spectra with a K(s) of 0.39 ± 0.10 μM. The partition ratio is ∼3, indicating potent inactivation that addition of e...

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Hlavní autoři: Nagy, Leslie D., Mocny, Catherine S., Diffenderfer, Laura E., Hsi, David J., Butler, Brendan F., Arthur, Evan J., Fletke, Kyle J., Palamanda, Jairam R., Nomeir, Amin A., Furge, Laura Lowe
Médium: Artigo
Jazyk:Inglês
Vydáno: The American Society for Pharmacology and Experimental Therapeutics 2011
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On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC3100908/
https://ncbi.nlm.nih.gov/pubmed/21422192
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1124/dmd.110.037630
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