Contents
Preface v
Contributors xiii
1 pKa, Solubility and Lipophilicity: Assessing
Physicochemical Properties of Lead Compounds
Yushen Guo and Hong Shen x
2 Use of Caco-2 Cell Monolayers to Study Drug Absorption
and Metabolism
Ming Hu, Jie Ling, Huimin Lin, and Jun Chen xx
3 Absorption Screening Using the PAMPA Approach
Jeffrey A. Ruell and Alex Avdeef xx
4 In Situ Single-Pass Perfused Rat Intestinal Model
for Absorption and Metabolism
Eun Ju Jeong, Yan Liu, Huimin Lin, and Ming Hu xx
5 In Vitro Permeation Study with Bovine Brain Microvessel Endothelial Cells
Sung-Hack Lee, Seong-Hee Park, Yaming Su,
and Patrick J. Sinko xx
6 An Enzymatic Microplate Assay for Testing P-glycoprotein Substrates and
Inhibitors
S. Orlowski, J. Nugier and Eric Ezan xx
7 Evaluation of Drug-Transporter Interactions Using In Vitro Cell Models
Yaming Su and Patrick J. Sinko xx
8 Plasma Protein-Binding Methods in Drug Discovery
Lucinda H. Cohen xx
9 Isothermal Titration Calorimetry Characterization
of Drug-Binding Energetics to Blood Proteins
Gary W. Caldwell and Zhengyin Yan xx
10 Metabolic Stability Assessed by Liver Microsomes
and Hepatocytes
David C. Ackley, Kevin T. Rockich,
and Timothy R. Baker xx
11 In Vitro Drug Metabolite Profiling Using Hepatic S9
and Human Liver Microsomes
Wu-Nan Wu and Linda A. McKown xxx
12 In Vitro Identification of UDP-glucuronosyltransferases
Involved in Drug Metabolism
Michael H. Court xxx
13 In Vitro CYP Induction in Human Hepatocytes
Daniel R. Mudra and Andrew Parkinson xxx
14 High-Throughput Screening of Human Cytochrome P450 Inhibitors Using
Fluorometric Substrates: Methodology
for 25 Enzyme/Substrate Pairs
David M. Stresser xxx
15 Evaluation of Cytochrome P450 Inhibition in Human Liver Microsomes
Zhengyin Yan and Gary W. Caldwell xxx
16 Identification of CYP Mechanism-Based Inhibitors
Amin A. Nomeir, Jairam Palamanda,
and Leonard Favreau xxx
17 Detection of DNA Adducts by 32P-Postlabeling Analysis
Naomi Suzuki, Padmaja M. Prabhu,
and Shinya Shibutani xxx
18 Covalent DNA Adduct Formation Mediated
by Cytochrome P450
Marie Stiborová xxx
19 Application of In Vitro Comet Assay for Genotoxicity
Testing
Bojana Zegura and Metka Filipic xxx
20 Assessing DNA Damage Using a Reporter Gene System
Xuming Jia and Wei Xiao xxx
21 Improvement of the Ames Test Using Human Liver S9
Preparation
Atsushi Hakura, Satoshi Suzuki, and Tetsuo Satoh xxx
22 Screening for Chemical Mutagens Using the Mouse
Lymphoma Assay
Tao Chen and Martha M. Moore xxx
23 A High Throughput Binding Assay for HERG
Keith Finlayson and John Sharkey xxx
24 In Vitro Drug Metabolism: Thiol Conjugation
Wei Tang and Randy R. Miller xxx
25 In Vitro Screening Assay of the Reactivity of Acyl
Glucuronides
Sébastien Bolze xxx
Index xxx