Results 221 to 230 of about 103,612 (260)
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Development of an in vitro incubation procedure for screening of CYP2D6 intrinsic clearance
Journal of Chromatography B, 2007The in vitro intrinsic clearances (CL(int)) for the metabolism of p-methoxymethamphetamine (PMMA) and fluoxetine by the CYP2D6 enzyme were calculated using a steady-state (SS) approach and a new general enzyme (GE) method, which measures the formation of product and the depletion of substrate as a function of time.
Sarah E G, Porter +2 more
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Environmental Science & Technology, 2016
The use of trophic magnification factors (TMFs) to characterize the bioaccumulation potentials of chemicals was encouraged; however, the method for the assessment of trophic magnification potentials is still lacking. We optimized the in vitro assays used for the measurement of intrinsic clearance in liver microsomes by incorporating benzo[a]pyrene (B(a)
Zheng, Guomao, Wan, Yi, Hu, Jianying
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The use of trophic magnification factors (TMFs) to characterize the bioaccumulation potentials of chemicals was encouraged; however, the method for the assessment of trophic magnification potentials is still lacking. We optimized the in vitro assays used for the measurement of intrinsic clearance in liver microsomes by incorporating benzo[a]pyrene (B(a)
Zheng, Guomao, Wan, Yi, Hu, Jianying
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In Silico Categorization of in Vivo Intrinsic Clearance Using Machine Learning
Molecular Pharmaceutics, 2013Machine learning has recently become popular and much used within the life science research domain, e.g., for finding quantitative structure-activity relationships (QSARs) between molecular structures and different biological end points. In the work presented here, we have applied orthogonal partial least-squares (OPLS), principal component analysis ...
Ya-Wen, Hsiao +2 more
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Drug Metabolism and Disposition, 2005
Due to the time-dependent loss of cytochrome P450 (P450)-mediated metabolism in freshly isolated hepatocytes, several types of culture systems have been developed to extend their lifespan. The aim of this study was to evaluate the ability of monolayer cultures of rat hepatocytes to determine the in vitro CL(int) compared with suspensions of freshly ...
Griffin, Sarah J., Houston, J. Brian
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Due to the time-dependent loss of cytochrome P450 (P450)-mediated metabolism in freshly isolated hepatocytes, several types of culture systems have been developed to extend their lifespan. The aim of this study was to evaluate the ability of monolayer cultures of rat hepatocytes to determine the in vitro CL(int) compared with suspensions of freshly ...
Griffin, Sarah J., Houston, J. Brian
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Prediction of hepatic extraction ratio from in vitro measurement of intrinsic clearance.
The Journal of Pharmacology and Experimental Therapeutics, 1977Under first-order conditions the activity of the hepatic drug-metabolizing enzymes may be closely approximated by the ratio of the in vitro kinetic constants Vmax and Km, which in turn is equivalent to the intrinsic clearance of the drug. In theory, after appropriate consideration for liver weight, blood flow and rug binding in the blood, the intrinsic
A, Rane, G R, Wilkinson, D G, Shand
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Xenobiotica, 2010
Intrinsic clearance (CL(int)) of seven probe cytochrome P450 substrates, across a wide range of clearance, was compared in microsomes and cryopreserved hepatocytes from the same four livers. Previous comparisons have shown system dependence, but using preparations from different donor livers.
Foster, Joanne A. +2 more
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Intrinsic clearance (CL(int)) of seven probe cytochrome P450 substrates, across a wide range of clearance, was compared in microsomes and cryopreserved hepatocytes from the same four livers. Previous comparisons have shown system dependence, but using preparations from different donor livers.
Foster, Joanne A. +2 more
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Journal of Pharmacokinetics and Biopharmaceutics, 1984
The influence of protein binding on the extraction ratio, and availability, of diazepam has been examined in the single-pass isolated perfused rat liver preparation. Binding of diazepam was varied by adjusting the concentration of albumin in the perfusate. In the absence of binding the extraction ratio of diazepam was high, 0.93-0.995.
M, Rowland +3 more
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The influence of protein binding on the extraction ratio, and availability, of diazepam has been examined in the single-pass isolated perfused rat liver preparation. Binding of diazepam was varied by adjusting the concentration of albumin in the perfusate. In the absence of binding the extraction ratio of diazepam was high, 0.93-0.995.
M, Rowland +3 more
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Journal of Hepatology, 1985
Child-Turcotte classification (CTC) is an empirical but widely accepted approach for assessment of severity of cirrhosis. However, it is not known to what extent CTC reflects accurately the degree of impairment of hepatic function. In this study we compared CTC, standard liver tests and intrinsic hepatic clearance (IHC) of indocyanine green as means of
J C, Barbare +5 more
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Child-Turcotte classification (CTC) is an empirical but widely accepted approach for assessment of severity of cirrhosis. However, it is not known to what extent CTC reflects accurately the degree of impairment of hepatic function. In this study we compared CTC, standard liver tests and intrinsic hepatic clearance (IHC) of indocyanine green as means of
J C, Barbare +5 more
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European Journal of Clinical Investigation, 1992
Abstract. Intrinsic hepatic clearance (K) of indocyanine green (ICG) is used as a quantitative measure of liver function. ICG is tightly bound to plasma proteins. The purpose of this study was to examine the effect of changes of plasma protein concentration on K. in anaesthetized pigs with intact hepatic circulation.
OTT P., KEIDING S., BASS L.
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Abstract. Intrinsic hepatic clearance (K) of indocyanine green (ICG) is used as a quantitative measure of liver function. ICG is tightly bound to plasma proteins. The purpose of this study was to examine the effect of changes of plasma protein concentration on K. in anaesthetized pigs with intact hepatic circulation.
OTT P., KEIDING S., BASS L.
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Drug Metabolism Letters, 2011
In contrast to human CYP2C9, non-human CYP2C enzymes do not appear to preferentially bind and metabolize anionic drugs. Using analogs of sulfaphenazole, the effect of an acidic sulfonamide group on apparent affinity and turnover rates was characterized with canine CYP2C21.
Charles W, Locuson +5 more
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In contrast to human CYP2C9, non-human CYP2C enzymes do not appear to preferentially bind and metabolize anionic drugs. Using analogs of sulfaphenazole, the effect of an acidic sulfonamide group on apparent affinity and turnover rates was characterized with canine CYP2C21.
Charles W, Locuson +5 more
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