Characterization of the Human Cytochrome P4502D6 Promoter
نویسندگان
چکیده
منابع مشابه
Extension of a predictive substrate model for human cytochrome P4502D6.
1. Metoprolol, indoramine, codeine, tamoxifen and prodipine, compounds which are clinically used, and MDMA (ecstasy) were fitted in a small molecule model for substrates of human cytochrome P4502D6. 2. For both the R- and S-enantiomer of metoprolol, the R- and S-enantiomer of MDMA, and for indoramine and codeine (all proven substrates of cytochrome P4502D6) an acceptable fit in the substrate mo...
متن کاملShort Communication The In Vitro Interaction of Dexmedetomidine with Human Liver Microsomal Cytochrome P4502D6 (CYP2D6)
The effect of dexmedetomidine (DEX) on cytochrome P4502D6 (CYP2D6)-dependent dextromethorphan O-demethylase (DEXTROase) activity was studied using native human liver microsomes. DEX (0.01–4.0 mM) inhibited DEXTROase activity (IC50 5 1.8 6 0.25 mM; mean 6 SD; N 5 5 livers) and was less potent than quinidine (QND), a prototypical and clinically relevant CYP2D6 inhibitor (IC50 5 0.22 6 0.02 mM; me...
متن کاملThe in vitro interaction of dexmedetomidine with human liver microsomal cytochrome P4502D6 (CYP2D6).
The effect of dexmedetomidine DEX on cytochrome P4502D6 (CYP2D6)-dependent dextromethorphan O-demethylase (DEXTROase) activity was studied using native human liver microsomes. DEX (0.01-4.0 microM inhibited DEXTROase activity (IC50 = 1.8 +/- 0.25 microM; mean +/- SD; N = 5 livers) and was less potent than quinidine (QND), prototypical and clinically relevant CYP2D6 inhibitor (IC50 = 0.22 +/- 0....
متن کاملShort Communication The In Vitro Interaction of Dexmedetomidine with Human Liver Microsomal Cytochrome P4502D6 (CYP2D6)
The effect of dexmedetomidine (DEX) on cytochrome P4502D6 (CYP2D6)-dependent dextromethorphan O-demethylase (DEXTROase) activity was studied using native human liver microsomes. DEX (0.01–4.0 mM) inhibited DEXTROase activity (IC50 5 1.8 6 0.25 mM; mean 6 SD; N 5 5 livers) and was less potent than quinidine (QND), a prototypical and clinically relevant CYP2D6 inhibitor (IC50 5 0.22 6 0.02 mM; me...
متن کاملPharmacogenetics of cytochrome p4502D6: genetic background and clinical implication.
Interindividual differences in the pharmacokinetics of a number of drugs are often due to hereditary polymorphisms of drug-metabolizing enzymes. Most important is cytochrome p4502D6 (CYP2D6), also known as debrisoquine/sparteine hydroxylase. It catalyzes hydroxylation or demethylation of more than 20% of drugs metabolized in the human liver, such as neuroleptics, antidepressants, some beta-bloc...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 1996
ISSN: 0021-9258
DOI: 10.1074/jbc.271.41.25269