Optimization in Drug Discovery : In Vitro Methods - Caldwell, Gary W.; Yan, Zhengyin; SpringerLink (Online service) (Totowa, NJ : Humana Press : Imprint: Humana, 2014)
Small Molecule Formulation Screening Strategies in Drug Discovery -- Assessment of Drug Plasma Protein Binding in Drug Discovery -- Drug Partition in Red Blood Cells -- Permeability Assessment Using 5-Day Cultured Caco-2 Cell Monolayers -- In Situ Single Pass Perfused Rat Intestinal Model -- Metabolic Stability Assessed by Liver Microsomes and Hepatocytes -- Metabolic Assessment in Alamethicin-Activated Liver Microsomes: Co-Activating CYPs and UGTs -- Phenotyping UDP-Glucuronosyltransferases (UGTs) Involved in Human Drug Metabolism: An Update -- In Vitro CYP/FMO Reaction Phenotyping -- Human Pregnane X Receptor (hPXR) Activation Assay in Stable Cell Lines -- Characterization of Constitutive Androstane Receptor (CAR) Activation -- DNA Binding (Gel Retardation Assay) Analysis for Identification of Aryl Hydrocarbon (Ah) Receptor Agonists and Antagonists -- Cell-Based Assays for Identification of Aryl Hydrocarbon Receptor (AhR) Activators -- In Vitro CYP Induction Using Human Hepatocytes -- Assessment of CYP3A4 Time-Dependent Inhibition in Plated and Suspended Human Hepatocytes -- Evaluation of Time-Dependent CYP3A4 Inhibition Using Human Hepatocytes -- Rapidly Distinguishing Reversible and Time-Dependent CYP450 Inhibition Using Human Liver Microsomes, Co-Incubation, and Continuous Fluorometric Kinetic Analyses -- Identification of Time-Dependent CYP Inhibitors Using Human Liver Microsomes (HLM) -- CYP Time-Dependent Inhibition (TDI) Using an IC50 Shift Assay with Stable Isotopic Labeled Substrate Probes to Facilitate Liquid Chromatography/Mass Spectrometry Analyses -- Screening for P-Glycoprotein (Pgp) Substrates and Inhibitors -- In Vitro Characterization of Intestinal Transporter, Breast Cancer Resistance Protein (BCRP) -- In Vitro Characterization of Intestinal and Hepatic Transporters: MRP2 -- In Vitro Characterization of Hepatic Transporters OATP1B1 and OATP1B3 -- In Vitro Characterization of Renal Transporters OAT1, OAT3, and OCT2 -- General Guidelines for Setting Up an In Vitro LC/MS/MS Assay -- Metabolite Identification in Drug Discovery -- Drug, Lipid, and Acylcarnitine Profiling Using Dried Blood Spot (DBS) Technology in Drug Discovery -- In Vitro Trapping and Screening of Reactive Metabolites Using Liquid Chromatography-Mass Spectrometry -- Quantitative Assessment of Reactive Metabolites -- In Vitro Assessment of the Reactivity of Acyl Glucuronides -- In Vitro COMET Assay for Testing Genotoxicity of Chemicals -- Assessing DNA Damage Using a Reporter Gene System -- Improved AMES Test for Genotoxicity Assessment of Drugs: Preincubation Assay Using a Low Concentration of Dimethyl Sulfoxide -- Methods for Using the Mouse Lymphoma Assay to Screen for Chemical Mutagenicity and Photo-Mutagenicity.
Keywords: Pharmacology; Pharmacology/Toxicology.