AIMC Topic: Microsomes, Liver

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Effect of Wuziyanzong pill on metabolism of dapoxetine in vivo and in vitro.

Journal of pharmaceutical and biomedical analysis Dec 15, 2018
In vitro incubation of rat liver microsomes with 30 μL of 100 μmol·L dapoxetine and 30 μL of 10, 100, 250, 500, 1000, 2500, or 5000 μg·mL Wuziyanzong pill was performed at 37 °C for 60 min. Dapoxetine concentration was analyzed by high performance li...
Naphthalenes Chromatography, High Pressure Liquid Rats Tandem Mass Spectrometry Benzylamines Microsomes, Liver Drugs, Chinese Herbal Herb-Drug Interactions Animals Inhibitory Concentration 50 Male
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Data Curation can Improve the Prediction Accuracy of Metabolic Intrinsic Clearance.

Molecular informatics Sep 24, 2018
A key consideration at the screening stages of drug discovery is in vitro metabolic stability, often measured in human liver microsomes. Computational prediction models can be built using a large quantity of experimental data available from public da...
Humans Machine Learning Databases, Chemical Metabolic Clearance Rate Hepatobiliary Elimination Drug Discovery Microsomes, Liver
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Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis.

European journal of medicinal chemistry Dec 28, 2017
Bruton's tyrosine kinase (Btk) is a Tec family kinase with a well-defined role in the B cell receptor (BCR) and Fcγ receptor (FcR) signaling pathways, which makes it a uniquely attractive target for the treatment of autoimmune diseases, such as rheum...
Haplorhini Pyrroles Pyrimidines Agammaglobulinaemia Tyrosine Kinase Mice Arthritis, Rheumatoid Cell Proliferation Rats, Sprague-Dawley Rats Animals Drug Design Humans Models, Molecular Molecular Structure Microsomes, Liver Protein Kinase Inhibitors Protein-Tyrosine Kinases Dogs Dose-Response Relationship, Drug Structure-Activity Relationship Cell Line
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Identification and characterization of the structure-activity relationships involved in UGT1A1 inhibition by anthraquinone and dianthrone constituents of Polygonum multiflorum.

Scientific reports Dec 20, 2017
The adverse effects of Polygonum (P.) multiflorum, including abnormal bilirubin metabolism, are a serious public health issue. As uridine diphosphate (UDP)-glucuronosyltransferase 1A1 (UGT1A1) is the only enzyme responsible for bilirubin metabolism, ...
Plant Roots Chromatography, High Pressure Liquid Rats, Sprague-Dawley Structure-Activity Relationship Glycosides Fallopia multiflora Glucuronosyltransferase Microsomes, Liver Anthraquinones Animals Male Plant Extracts Rats In Vitro Techniques
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Predicting Mouse Liver Microsomal Stability with "Pruned" Machine Learning Models and Public Data.

Pharmaceutical research Sep 28, 2015
PURPOSE: Mouse efficacy studies are a critical hurdle to advance translational research of potential therapeutic compounds for many diseases. Although mouse liver microsomal (MLM) stability studies are not a perfect surrogate for in vivo studies of m...
Small Molecule Libraries Databases, Pharmaceutical Principal Component Analysis Bayes Theorem Models, Biological Microsomes, Liver Drug Discovery Pharmaceutical Preparations Machine Learning Mice Animals
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Metabolite Profiling of ADB-FUBINACA, A New Synthetic Cannabinoid.

Current neuropharmacology Jul 1, 2017
Metabolite profiling of novel psychoactive substances (NPS) is critical for documenting drug consumption. N-(1-amino-3,3-dimethyl-1-oxobutan-2-yl)-1-(4-fluorobenzyl)-1H-indazole-3-carboxamide (ADB-FUBINACA) is an emerging synthetic cannabinoid whose ...
Psychotropic Drugs Humans Metabolome Biomarkers In Vitro Techniques Microsomes, Liver Indazoles
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