2024 Phenacetin o-deethylase

Phenacetin o-deethylase

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WebApr 1, 1996 · These metabolic reactions were: 7-ethoxyresorufin O-deethylation (CYP1A1), phenacetin O-deethylation (CYP1A2), coumarin 7-hydroxylation (CYP2A6), tolbutamide 4-methylhydroxylation… View on PubMed Save to Library Create Alert Cite 393 Citations Citation Type More Filters WebNov 6, 2013 · PL only decreased CYP 1A2-catalyzed phenacetin O -deethylase activity with IC 50 values of 10.0 μM, whereas the IC 50 of PL on CYP1A1-catalyzed phenacetin O -deethylase activity was fivefold higher than the value of CYP1A2 (Fig. 4 ). Accordingly, PL was a specific substrate having inhibitory effects on the CYP1A2 in HLMs, not CYP1A1. …

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WebPhenacetin O-deethylation, widely used as an index reaction for cytochrome P450 1A2 (CYP1A2) activity, displays biphasic kinetics in human liver microsomes. CYP1A2 has … WebJul 1, 1995 · L-754,394 is a potent and specific inhibitor of the HIV-1 encoded protease that is essential for the maturation of the infectious virus. The drug exhibited dose-dependent kinetics in all species studied (rat, dog and monkey); the apparent clearance decreased when the dose was increased. northey avenue playing fields

In Vitro Comparison of Cytochrome P450-Mediated Metabolic Activities …

WebNov 2, 2010 · Samples were phenotyped for phenacetin O -deethylase activity, and the expression of CYP1A2 protein and mRNA was determined. CYP1A2 expression and function was increased in smokers and decreased in patients with inflammation and cholestasis. WebHuman cytochrome P-450PA (P-450IA2), the phenacetin O-deethylase, is primarily responsible for the hepatic 3-demethylation of caffeine and N-oxidation of carcinogenic arylamines. M AButler, MIwasaki, F PGuengerich, and F FKadlubarAuthors Info & … Web1. Phenacetin 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 … northey and northey

Human cytochrome P-450PA (P-450IA2), the phenacetin O-deethylase…

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WebThe activity of 7-ethoxycoumarin O-deethylase (ECOD) has been measured in liver biopsy samples from 23 patients (smokers and non-smokers) with different degrees of structural liver damage. The results, which reflect in vitro cytochrome P450-dependent biotransformation, were correlated with various measures of the P450-dependent in vivo … WebSep 1, 1997 · [O-ethyl 14C]phenacetinO-deethylase ANF 7, 8-benzoflavone FURA furafylline COUM coumarin IC 50 concentration of drug required to inhibit activity by 50% K apparent inhibition constant (dissociation constant of the enzyme-inhibitor, or EI, complex) K m apparent Michaelis constant Vmax apparent maximal initial reaction velocity north extended stay mishawaka in northey brothers builders

"WebPhenacetin (acetophenetidin, N-(4-ethoxyphenyl)acetamide) is a pain-relieving and fever-reducing drug, which was widely used following its introduction in 1887. It was withdrawn … " - Phenacetin o-deethylase

Phenacetin o-deethylase

WebPhenacetin, a painkiller, was the world’s first synthetic pharmaceutical drug. It was one of the first painkillers that was not derived from opium while at the same time being absent … WebO-deethylase activity in rat liver microsomes by antofloxacin. (B) The corresponding double reciprocal plot of the rates of inactivation as a function of antofloxacin concentration.

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Webzymatic assay assessed phenacetin O-deethylase (a CYP1A2 substrate) activity by measuring the CYP1A2-dependent metabolite acetaminophen in supernatants. Acetaminophen was quantified using liquid chromatography coupled with tandem mass spectrometry(LC-MS/MS). For enzyme activity measurement, the criteria for Webphenacetin 0-deethylation has been described, with 5-10% of the population deficient in this activity (22). [The evidence that human P-450PA, the phenacetin 0-deethylase, is the …

WebPhenacetin O-deethylation by human liver microsomes in vitro: inhibition by chemical probes, SSRI antidepressants, nefazodone and venlafaxine L. L. von Moltke, David J. … WebJan 1, 2013 · In HLMs, mollugin inhibited phenacetin O -deethylase activity with IC 50 values of 1.03 and 5.33 μM, without and with pre-incubation, respectively. The results indicated that mollugin has a typical pattern of competitive inhibition mode for CYP1A2 enzyme. From the Lineweaver–Burk plot, the Ki value was calculated to be 3.74 μM in HLMs.

WebNational Center for Biotechnology Information WebAbstract. Olfactory rosettes from trout (Salmo gairdneri) were found to metabolise (14C-ethyl)-phenacetin to 14CO2 in vitro. Based on wet weight, the rate of metabolism was …

WebThe inhibitory effects of mexiletine and 10 antiarrhythmic drugs on phenacetin O-deethylation, a marker reaction of CYP1A2, ... The current in vitro study using human liver microsomes showed that, among eleven antiarrhythmics, mexiletine inhibited phenacetin O-deethylase activity in human liver microsomes with an IC 50 value less than 40 μm ...

WebNov 7, 2003 · Phenacetin O -deethylation activity The microsomal phenacetin O -deethylation activity was determined by measuring the rate of paracetamol formation at 37° C by a modification of a high-performance liquid chromatography (h.p.l.c.) method reported previously [ 32 ]. how to save as a vector file in illustratorWebPhenacetin O-deethylase differs from another cytochrome P-450 enzyme that shows genetic polymorphism, debrisoquine 4-hydroxylase , in molecular mass, amino acid … how to save as a tiff fileWeb456211 CYP1A1 + reductase 7-Ethoxyresorufin O-deethylase 0.5 nmol P450 in 0.5 mL 456203 CYP1A2 + reductase Phenacetin O-deethylase 0.5 nmol P450 in 0.5 mL 456220 CYP1B1 + reductase 7-Ethoxyresorufin O-deethylase 0.5 nmol P450 in 0.5 mL 456204 CYP2A6 + reductase Coumarin 7-hydroxylase 1 nmol P450 in 0.5 mL 456254 CYP2A6 + … northey avenueWebFeb 1, 1990 · Phenacetin is metabolized primarily by O-deethylation to paracetamol (POD activity), a reaction catalysed by cytochrome P450. The high affinity component of POD … northey arms box menuWebBiotransformation of phenacetin via O-deethylation to acetaminophen, an index reaction reflecting activity of Cytochrome P450-1A2, was studied in microsomal preparations from … northey arms menuWebOct 1, 1997 · Seven selective catalytic activity markers for cytochrome P450-mediated reactions were measured: phenacetin O -deethylase (P4501A1/2), coumarin 7-hydroxylase (P4502A6), tolbutamide hydroxylase (P4502C8/9), S -mephenytoin 4′-hydroxylase (P4502C19), dextromethorphan O- demethylase (P4502D6), chlorzoxazone 6-hydroxylase … nor they areWebJan 1, 2000 · This study was conducted to identify the cytochrome P-450 (CYP) isoform (s) responsible for the pimobendan O -demethylation in human liver microsomes. Pimobendan O -demethylase activity in human liver microsomes was significantly correlated with phenacetin O -deethylase activity. northey arms box bath