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Metabolites formation

The concentration of a metabolite (Cm), too, follows such a bi-exponential kinetics depending on the metabolite formation rate constant (Kmet). [Pg.956]

Reactive Metabolite Formation, Mechanism-Based CYP Inhibition,... [Pg.142]

Figure 9.11 Examples of P450 reactions important in metabolite formation... Figure 9.11 Examples of P450 reactions important in metabolite formation...
Another important factor to evaluate is the initial dye concentration of the azo dye-containing wastewaters. Swshadri and Bishop drew a conclusion that dye concentration may cause a drop in the percentage of dye removal. Furthermore, the inhibition may be directly related to the effects of increased dye metabolite formation due to higher dye concentrations. Cariell et al. [96] found that C.I. Reactive Red 141 was inhibitory to anaerobic organisms at concentrations greater than 100 mg/L. [Pg.149]

Ortiz de Montellano PR, Komives EA. Branchpoint for heme alkylation and metabolite formation in the oxidation of arylacetylenes by cytochrome P-450. J Biol Chem 1985 260(6) 3330-3336. [Pg.108]

Mansuy D, Valadon P, Erdelmeier I, et al. Thiophene S-oxides as new reactive metabolites formation by cytochrome P450 dependent oxidation and reaction with nucleophiles. J Am Chem Soc 1991 113(20) 7825—7826. [Pg.165]

Stereoisomerism will influence metabolism and toxicity. For example, Lu et al. (1998) reported a comparison of (5)-(—jlfosfamide and (i )-(+)-Ifsosfamide. They demonstrated that there were significant differences between the two stereoisomers with regard to pharmacokinetic behavior and major metabolite formation, as shown in Table 18.13. [Pg.733]

Gentest (now BD Biosciences) was the first to develop spectrophotometric assays to study CYP inhibition [98]. These assays are based on the turnover of mildly fluorescent substrate probes to moderately fluorescent metabolites, where metabolite formation is monitored by an increase in fluorescence using a plate reader [99,100]. Problems with these methods include background interference due to low signal-to-noise ratio, chemotype-specific interference and fluorescence quenching. Aurora Biosciences (now Vertex) has designed probes that exhibit larger fluorescence... [Pg.204]

In studies of the fate of hydrocarbons in terrestrial animals, considerable attention is directed toward relations between aromatic hydrocarbon metabolism, interactions of metabolites with macromolecules (e.g., DNA), and the formation of neoplastic lesions (] ). A broad perspective exists in studies with marine organisms. In the aquatic forms, exposure to pollutants that are rich in aromatic hydrocarbons, such as petroleum, leads to a wide variety of acute and chronic effects (2J. Attempts to delineate these effects require an understanding of the accumulation of the xenobiotics in tissues and an assessment of metabolite formation and retention. The important additional problem of the interaction of metabolites with genetic materials has not been studied to an appreciable degree in marine life. [Pg.57]

A screening of about 40 strains currently used for steroid hydroxylation was undertaken, using reverse-phase HPLC and UV absorption to detect and quantitate metabolite formation. Most of the strains tested were able to metabolize extensively this substrate within a 1- to 5-day period, producing in the incubation medium variable amounts of at least eight hydroxylated metabolites (80-87), essentially depending on the strain used [189]. [Pg.204]

As a first approximation, we consider the main subsurface transformation processes to comprise reactions leading to chemical transformation or degradation and metabolite formation in the liquid phase or the solid-liquid interface and reactions resulting in complexation of chemicals, which in turn lead to a change in their physicochemical properties. [Pg.271]

The absorption and excretion of carbenicillin in man has been reported [396]. The antibiotic is not absorbed intact from the gut intramuscular injection (which is painful) often provides adequate serum levels (approximately 20 Mg/ntl) but infections with Pseudomonas strains having minimum inhibitory concentrations up to, or higher than, 100 Mg/ml require intravenous thbrapy to achieve such levels. No evidence of active metabolite formation has been obtained. Marked reductions in the half-life (and serum levels) of carbenicillin follow extracorporeal dialysis or peritoneal dialysis, the former producing the most striking effect [397]. These results were, of course, obtained in patients with severe renal failure. Patients with normal renal function rapidly eliminate the drug but, as with all penicillins, renal tubular secretion can be retarded by concurrent administration of probenecid. [Pg.51]

Assessment of metabolic volume of distribution and metabolite formation ... [Pg.20]

Ju, C. andUetrecht, J.P. (2002) Mechanism of idiosyncratic drug reactions reactive metabolites formation, protein binding and the regulation of the immune system. Current Drug Metabolism, 3, 367-377. [Pg.162]

In early discovery determination of percent inhibition at a single concentration is sufficient to compare compounds vfithin a chemical series. Typically concentrations in the 1-5 j,M range are used [27, 28]. Test compounds and vehicle control are incubated with the probe substrate and the amount of metabolite formation from the probe substrate determined. The metabolic rate can then be expressed as a percentage of the... [Pg.172]


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See also in sourсe #XX -- [ Pg.228 ]




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