Phenacetin o-deethylase
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. 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 …
Phenacetin o-deethylase
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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, widely used as an index reaction for cytochrome P450 1A2 (CYP1A2) activity, displays biphasic kinetics in human liver microsomes. CYP1A2 has …
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 … 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 ].
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 ... 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.
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 …
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 jobs marketing media \u0026 communicationsWebAbstract. 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 … int a 1WebThe 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 … int a 1000 初始化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 … int a 100 0 什么意思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 & … jobs.marksandspencer.comWebPhenacetin O-deethylation by human liver microsomes in vitro: inhibition by chemical probes, SSRI antidepressants, nefazodone and venlafaxine L. L. von Moltke, David J. … jobs maricopa community collegeWebPhenacetin O-deethylase differs from another cytochrome P-450 enzyme that shows genetic polymorphism, debrisoquine 4-hydroxylase , in molecular mass, amino acid … int a 100 10*10