Intrinsic Clearance and Metabolism Pathway of Fosthiazate in Rat and Cock Liver Microsomes: From Chiral Assessment View.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of agricultural and food chemistry"
DOI: 10.1021/acs.jafc.1c05217
Abstract: Chiral fosthiazate enters the organisms via environmental exposure and food web enrichment. Liver subcellular fractions of rats (RLM) and cocks (CLM) were prepared to explore the stereoselective metabolism of fosthiazate in vitro. The results indicated… read more here.
Keywords: clearance metabolism; metabolism; fosthiazate fosthiazate; fosthiazate ... See more keywords
Multispecies Machine Learning Predictions of In Vitro Intrinsic Clearance with Uncertainty Quantification Analyses.
Sign Up to like & getrecommendations! Published in 2022 at "Molecular pharmaceutics"
DOI: 10.1021/acs.molpharmaceut.2c00680
Abstract: In pharmaceutical research, compounds are optimized for metabolic stability to avoid a too fast elimination of the drug. Intrinsic clearance (CLint) measured in liver microsomes or hepatocytes is an important parameter during lead optimization. In… read more here.
Keywords: uncertainty; machine learning; intrinsic clearance; clint ... See more keywords
Reliability of In Vitro Methods Used to Measure Intrinsic Clearance of Hydrophobic Organic Chemicals by Rainbow Trout: Results of an International Ring Trial
Sign Up to like & getrecommendations! Published in 2018 at "Toxicological Sciences"
DOI: 10.1093/toxsci/kfy113
Abstract: Abstract In vitro assays are widely employed to obtain intrinsic clearance estimates used in toxicokinetic modeling efforts. However, the reliability of these methods is seldom reported. Here we describe the results of an international ring… read more here.
Keywords: results international; used measure; ring trial; international ring ... See more keywords
Evaluation of the Disconnect between Hepatocyte and Microsome Intrinsic Clearance and In Vitro In Vivo Extrapolation Performance
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DOI: 10.1124/dmd.120.000131
Abstract: The use of in vitro in vivo extrapolation (IVIVE) from human hepatocyte (HH) and human liver microsome (HLM) stability assays is a widely accepted predictive methodology for human metabolic clearance (CLmet). However, a systematic underprediction… read more here.
Keywords: vitro vivo; hlm; clearance; vivo extrapolation ... See more keywords
Effects of CYP2C19 Variants on Fluoxetine Metabolism in vitro
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DOI: 10.1159/000475598
Abstract: Aims: CYP2C19 is an important member of the cytochrome P450 enzyme superfamily. We recently identified 31 CYP2C19 alleles in the Han Chinese population. The aim of this study was to assess the catalytic activities of… read more here.
Keywords: cyp2c19 variants; vitro; effects cyp2c19; cyp2c19 ... See more keywords
Effects of CYP2C19 variants on the metabolism of tapentadol in vitro
Sign Up to like & getrecommendations! Published in 2022 at "Iranian Journal of Basic Medical Sciences"
DOI: 10.22038/ijbms.2022.56996.12710
Abstract: Objective(s): This study aims to evaluate the catalytic activities of 31 CYP2C19 alleles and their effects on the metabolism of tapentadol in vitro. Materials and Methods: Insect microsomes expressing the CYP2C19 alleles were incubated with… read more here.
Keywords: metabolism; intrinsic clearance; cyp2c19; tapentadol vitro ... See more keywords