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Optimization In Drug Discovery
by Gary W. Caldwell
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Table Of Contents
1. pKa, Solubility, and Lipophilicity : Assessing Physicochemical Properties of Lead Compounds
2. Use of Caco-2 Cell Monolayers to Study Drug Absorption and Metabolism
3. Absorption Screening Using the PAMPA Approach
4. In Situ Single-Pass Perfused Rat Intestinal Model for Absorption and Metabolism
5. In Vitro Permeation Study With Bovine Brain Microvessel Endothelial Cells
6. An Enzymatic Microplate Assay for Testing P-Glycoprotein Substrates and Inhibitors
7. Evaluation of Drug-Transporter Interactions Using In Vitro Cell Models
8. Plasma Protein-Binding Methods in Drug Discovery
9. Isothermal Titration Calorimetry Characterization of Drug-Binding Energetics to Blood Proteins.
10. Metabolic Stability Assessed by Liver Microsomes and Hepatocytes
11. In Vitro Drug Metabolite Profiling Using Hepatic S9 and Human Liver Microsomes
12. In Vitro Identification of UDP-Glucuronosyl transferases Involved in Drug Metabolism
13. In Vitro CYP Induction in Human Hepatocytes
14. High-Throughput Screening of Human Cytochrome P450 Inhibitors Using Fluorometric Substrates : Methodology for 25Enzyme/Substrate Pairs
15. Evaluation of Cytochrome P450 Inhibition in Human Liver Microsomes
16. Identification of CYP Mechanism-Based Inhibitors
17. Detection of DNA Adducts by 32P-Postlabeling Analysis
18. Covalent DNA Adduct Formation Medicated by Cytochrome P450
19. Application of In Vitro Comet Assay for Genotoxicity Testing
20. Assessing DNA Damage Using a Reporter Gene System
21. Improvement of the Ames Test Using Human Liver S9 Preparation
22. Screening for Chemical Mutagens Using the Mouse Lymphoma Assay
23. A High-Throughput Binding Assay for HERG
24. In Vitro Drug Metabolism: Thiol Conjugation
25. In Vitro Screening Assay of the Reactivity of Acyl GlucuronidesISBN - 9788184894844
Pages : 440
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