Optimization in Drug Discovery In Vitro Methods

Thoroughly revised and updated, Optimization in Drug Discovery: In Vitro Methods, Second Edition presents a wide spectrum of in vitro assays including formulation, plasma binding, absorption and permeability, cytochrome P450 (CYP) and UDP-glucuronosyltransferases (UGT) metabolism, CYP inhibition and...

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Bibliographic Details
Other Authors: Caldwell, Gary W. (Editor), Yan, Zhengyin (Editor)
Format: eBook
Language:English
Published: Totowa, NJ Humana 2014, 2014
Edition:2nd ed. 2014
Series:Methods in Pharmacology and Toxicology
Subjects:
Online Access:
Collection: Springer eBooks 2005- - Collection details see MPG.ReNa
Table of Contents:
  • 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
  • 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 Characterization of Renal Transporters OAT1, OAT3, and OCT2
  • General Guidelines for Setting Upan 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