2024 Phenacetin o-deethylase

Phenacetin o-deethylase

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WebWe have now investigated the selectivity of inhibition of human monooxygenase activities by furafylline. 2. Furafylline was a potent, non-competitive inhibitor of high affinity phenacetin O-deethylase activity of microsomal fractions of human liver, a reaction catalysed by P450IA2, with an IC50 value of 0.07 microM. 3. 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.

Inhibitory effects of antiarrhythmic drugs on phenacetin O ...

WebPhenacetin O-deethylase differs from another cytochrome P-450 enzyme that shows genetic polymorphism, debrisoquine 4-hydroxylase , in molecular mass, amino acid … WebPhenacetin O-deethylation by human liver microsomes in vitro: inhibition by chemical probes, SSRI antidepressants, nefazodone and venlafaxine L. L. von Moltke, David J. … how do i dictate to word

Human Cytochrome P-450 PA (P-450IA2), the Phenacetin O …

Web[The evidence that human P-450PA, the phenacetin 0-deethylase, is the product of the human P450IA2 gene is as follows: antibodies raised to rat P-450ISF-G (P-450IA2) or human P-45OPA recognize a single polypeptide in human liver microsomes and inhibit microsomal phenacetin O-deethylase activity; the level of immunoreactive protein is highly cor- WebBiotransformation of phenacetin via O-deethylation to acetaminophen, an index reaction reflecting activity of Cytochrome P450-1A2, was studied in microsomal preparations from … 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. how do i die my hair

Phenacetin O-deethylation by human liver microsomes

Selective inhibitory effects of mollugin on CYP1A2 in human liver ...

WebJan 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. WebAbstract Phenacetin O-deethylase activity was impaired, both in vivo and in vitro, in poor metabolisers of debrisoquine, consistent with the work of others. No impairment was observed in the oxidation of acetanilide, amylobarbitone or antipyrine in the PM phenotype. how much is prime drink at costcoWebzymatic 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 how much is prime company worth

"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. … " - Phenacetin o-deethylase

Phenacetin o-deethylase

Inhibitory effects of antiarrhythmic drugs on phenacetin O ...

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 ... Web456211 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 + …

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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. 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 …

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 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 ].

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 WebDec 9, 2024 · The assays for the activities of phenacetin O -deethylase (CYP1A2), diclofenac 4′-hydroxylase (CYP2C9), and midazolam 1′-hydroxylase (CYP3A) in human or rat liver microsomes were performed following previously reported methods [ 20] …

WebFeb 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 …

WebPhenacetin O-deethylation, widely used as an index reaction for cytochrome P450 1A2 (CYP1A2) activity, displays biphasic kinetics in human liver microsomes. CYP1A2 has … how do i dim the adt pulse panel lightWebJun 8, 2000 · Phenacetin O‐deethylation, widely used as an index reaction for cytochrome P450 1A2 (CYP1A2) activity, displays biphasic kinetics in human liver microsomes. … how much is prime drink costWebHuman 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 & … how much is prime drink company worthWebThe 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 … how do i dim my screenWebJan 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. how do i dimension a solar thermal system ptcWebOct 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 … how much is prime csgoWebMay 22, 1992 · BUTLER, M.A., HUMAN 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 - (AROMATIC-AMINES HETEROCYCLIC AMINES CARCINOGEN METABOLISM), … how do i dim the light