Phenacetin o-deethylation
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. 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 …
Phenacetin o-deethylation
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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]- WebCytochrome P450 1A2 Messenger RNA is a More Reliable Marker than Cytochrome P450 1A2 Activity, Phenacetin O-Deethylation, for Assessment of Induction Potential of Drug …
WebAbstract. Phenacetin O-deethylation, widely used as an index reaction for cytochrome P450 1A2 (CYP1A2) activity, displays biphasic kinetics in human liver microsomes. CYP1A2 … WebAug 13, 2014 · Because phenacetin O -deethylation is specifically metabolized by CYP1A2 [ 36 ], the authors examined the correlation between 2,3,7-triCDD 8-hydroxylation and phenacetin O -deethylation in human liver microsomes.
WebThe 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) … WebMar 26, 2001 · This invention provides an improved computationally derived regression-based method for determining IC50 or EC50 values for chemical compounds, which predicts potential drug-drug interactions involving cytochrome P450 and other enzymes, transporters, receptors or proteins with active site (s).
WebJun 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 …
Webhydroxylation,a putative cytochrome P-4502E1activity,in 改变药物生物转化反应最常见的两种原因是CYP酶的诱导和抑制,酶的诱导可增加生物转化率,·50·从而降低药物的浓度,通常表现为药物的作用降低,若代谢形成活性药物则可增加药物的毒性;而酶的抑制可增加药物的浓度,延长药理作用时间,药物引起的毒性反应的发生率也会增加旧1。 芫花被中华人民共和国药典列 … lowes blue hawk shelvingWebSep 1, 1981 · Abstract. Human and rat liver microsomal fractions exhibit non-linear Michaelis-Menten kinetics in the O-deethylation of both phenacetin and 7 … lowes blue potslowes blue ridge pine smartcoreWebMolecules 2011, 16 6592 Keywords: corydaline; cytochrome P450 inhibition; UDP-glucuronosyltransferase inhibition; human liver microsomes; drug-drug interaction 1. Introduction Corydalis tubers, the roots of Corydalis yanhusuo W.T. Wang, have long been used as an herbal drug for their analgesic and anti-ulcer effects [1-3]. lowes blue painters tapeWebNov 1, 2011 · Phenacetin O-deethylation is the preferred probe reaction for CYP1A2, in which the metabolite, acetaminophen, is quantified using liquid chromatography-tandem … lowes blue rhino exchangeWebMar 1, 2002 · These results suggest that diclofenac 4-hydroxylation, dextromethorphan O-demethylation and midazolam 4-hydroxylation are useful as catalytic markers of CYP2C6, … lowes blue plastic tarpsWebMethods: Using pooled human liver microsomes, the in vitro inhibitory effects of isoniazid on CYP1A2 (phenacetin O-deethylation), CYP2A6 (coumarin 7-hydroxylation), CYP2C9 … lowes bluetooth lock