Phenacetin o-deethylation
WebAbstract. Phenacetin O-deethylation, widely used as an index reaction for cytochrome P450 1A2 (CYP1A2) activity, displays biphasic kinetics in human liver microsomes. CYP1A2 … WebSep 1, 1981 · Abstract. Human and rat liver microsomal fractions exhibit non-linear Michaelis-Menten kinetics in the O-deethylation of both phenacetin and 7 …
Phenacetin o-deethylation
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WebMar 31, 2024 · Phenacetin and nifedipine are substrates of CYP1A2 and CYP3A11, respectively. Both substrates are converted via the CYP enzyme to paracetamol and dehydronefedipine, respectively. The concentrations of paracetamol and dehydronefedipine were used to determine the activities of mCYP1A2 and mCYP3A11. Webjaceosidin potently inhibited CYP1A2-catalyzed phenacetin O-deethylation with 50% inhibitory concentration (IC50) values of 9.4 μM and 5.3 μM, respectively, and CYP2C9-catalyzed diclofenac 4-hydroxylation with IC50 values of 4.1 μM and 10.2 μM, respectively. Eupatilin and jaceosidin were also found to moderately inhibit CYP2C19-catalyzed [S]-
WebNine different concentrations of phenacetin, ranging from 1 to 200 μm, were used in the kinetic experiments for phenacetin O-deethylation by microsomes from three human … WebBiotransformation of phenacetin via O-deethylation to acetaminophen, an index reaction reflecting activity of Cytochrome P450-1A2, was studied in microsomal preparations from …
WebPhenacetin O-deethylation is the preferred probe reaction for CYP1A2, in which the metabolite, acetaminophen, is quantified using liquid chromatography-tandem mass spectrometry. DMSO was found to inhibit CYP1A2-mediated phenacetin O-deethylation even at low concentrations (0.1%). WebIn previous studies, the oxygen deethylation metabolism of phenacetin is often used to reflect the activity of CYP1A2. However, due to the potential toxicity of phenacetin, this …
WebJun 13, 2012 · Phenacetin is primarily metabolized to acetaminophen via O-deethylation, although the formation of a minor metabolite acetol (∼5%) via acetyl hydroxylation has …
WebMar 1, 2002 · These results suggest that diclofenac 4-hydroxylation, dextromethorphan O-demethylation and midazolam 4-hydroxylation are useful as catalytic markers of CYP2C6, … charlotte mason daily routinecharlotte mason gateleyWebJun 15, 2012 · Phenacetin O-deethylation is a marker reaction of cytochrome P4501A2 (CYP1A2) activity. In this study, our aim is to investigate whether phenacetin O … charlotte mason habit trainingWebJun 1, 2001 · Phenacetin O -deethylation (CYP1A2), coumarin 7-hydroxylation (CYP2A6), diclofenac 4′-hydroxylation (CYP2C9), omeprazole 5-hydroxylation (CYP2C19), dextromethorphan O -demethylation (CYP2D6), 7-ethoxy-4-trifluoromethylcoumarin deethylation (CYP2B6), p -nitrophenol hydroxylation (CYP2E1), and omeprazole … charlotte mason grammar curriculumWebThe in vitro inhibitory effects of gemfibrozil on cytochrome P450 (CYP) 1A2 (phenacetin O-deethylation), CYP2A6 (coumarin 7-hydroxylation), CYP2C9 (tolbutamide hydroxylation), CYP2C19 (S-mephenytoin 4'-hydroxylation), CYP2D6 (dextromethorphan O-deethylation), CYP2E1 (chlorzoxazone 6-hydroxylation), and CYP3A4 (midazolam 1'-hydroxylation) … charlotte mason home education pdfWebMethods: Using pooled human liver microsomes, the in vitro inhibitory effects of isoniazid on CYP1A2 (phenacetin O-deethylation), CYP2A6 (coumarin 7-hydroxylation), CYP2C9 … charlotte mason habit training curriculumWebPhenacetin O-deethylation catalysed by human liver microcomes has been examined over a substrate concentration range of 2.5 to 700 microM using preparations of eight human … charlotte mason homeschool curriculum free