Optimization in Drug Discovery: In Vitro Methods: 2014 (Methods in

Description: 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 induction, drug transporters, drug-drug interactions via assessment of reactive metabolites, genotoxicity, and chemical and photo-mutagenicity assays. Written for the Methods in Pharmacology and Toxicology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible protocols, and tips on troubleshooting and avoiding known pitfalls. Expert authors have developed and utilized these in vitro assays to achieve "drug-like" characteristics in addition to efficacy properties and good safety profiles of drug candidates. Comprehensive and up-to-date, Optimization in Drug Discovery: In Vitro Methods, Second Edition aims to guide researchers down the difficult path to successful drug discovery and development. 1. Small Molecule Formulation Screening Strategies in Drug Discovery Gary W. Caldwell, Becki Hasting, John Masucci, and Zhengyin Yan 2. Assessment of Drug Plasma Protein Binding in Drug Discovery Dennis Kalamaridis and Nayan Patel 3. Drug Partition in Red Blood Cells Dennis Kalamaridis and Karen DiLoreto 4. Permeability Assessment Using 5-Day Cultured Caco-2 Cell Monolayers Gary W. Caldwell, Chrissa Ferguson, Robyn Buerger, Lovonia Kulp, and Zhengyin Yan 5. In Situ Single Pass Perfused Rat Intestinal Model Maria Markowska and L. Mark Kao 6. Metabolic Stability Assessed by Liver Microsomes and Hepatocytes Kevin J. Coe and Tatiana Koudriakova 7. Metabolic Assessment in Alamethicin-Activated Liver Microsomes: Co-Activating CYPs and UGTs Gary W. Caldwell and Zhengyin Yan 8. Phenotyping UDP-Glucuronosyltransferases (UGTs) Involved in Human Drug Metabolism: An Update Michael H. Court 9. In Vitro CYP/FMO Reaction Phenotyping Carlo Sensenhauser 10. Human Pregnane X Receptor (hPXR) Activation Assay in Stable Cell Lines Judy L. Raucy 11. Characterization of Constitutive Androstane Receptor (CAR) Activation Caitlin Lynch, Haishan Li, and Hongbing Wang 12. DNA Binding (Gel Retardation Assay) Analysis for Identification of Aryl Hydrocarbon (Ah) Receptor Agonists and Antagonists Anatoly A. Soshilov and Michael S. Denison 13. Cell-Based Assays for Identification of Aryl Hydrocarbon Receptor (AhR) Activators Guochun He, Jing Zhao, Jennifer C. Brennan, Alessandra A. Affatato, Bin Zhao, Robert H. Rice, and Michael S. Denison 14. In Vitro CYP Induction Using Human Hepatocytes Monica Singer, Carlo Sensenhauser, and Shannon Dallas 15. Assessment of CYP3A4 Time-Dependent Inhibition in Plated and Suspended Human Hepatocytes J. George Zhang and David M. Stresser 16. Evaluation of Time-Dependent CYP3A4 Inhibition Using Human Hepatocytes Yuan Chen and Adrian J. Fretland 17. Rapidly Distinguishing Reversible and Time-Dependent CYP450 Inhibition Using Human Liver Microsomes, Co-Incubation, and Continuous Fluorometric Kinetic Analyses Gary W. Caldwell and Zhengyin Yan 18. Identification of Time-Dependent CYP Inhibitors Using Human Liver Microsomes (HLM) Kevin J. Coe, Judith Skaptason, and Tatiana Koudriakova 19. CYP Time-Dependent Inhibition (TDI) Using an IC50 Shift Assay with Stable Isotopic Labeled Substrate Probes to Facilitate Liquid Chromatography/Mass Spectrometry Analyses Gary W. Caldwell and Zhengyin Yan 20. Screening for P-Glycoprotein (Pgp) Substrates and Inhibitors Qing Wang and Tina M. Sauerwald 21. In Vitro Characterization of Intestinal Transporter, Breast Cancer Resistance Protein (BCRP) Chris Bode and Li-Bin Li 22. In Vitro Characterization of Intestinal and Hepatic Transporters: MRP2 Ravindra Varma Alluri, Peter Ward, Jeevan Kunta, Brian C. Ferslew, Dhiren R. Thakker, and Shannon Dallas 23. In Vitro Characterization of Hepatic Transporters OATP1B1 and OATP1B3 Blair Miezeiewski and Allison McLaughlin 24. In Vitro Characterization of Renal Transporters OAT1, OAT3, and OCT2 Ying Wang and Nicole Behler 25. General Guidelines for Setting Up an In Vitro LC/MS/MS Assay John A. Masucci and Gary W. Caldwell 26. Metabolite Identification in Drug Discovery Wing W. Lam, Jie Chen, Rongfang Fran Xu, Jose Silva, and Heng-Keang Lim 27. Drug, Lipid, and Acylcarnitine Profiling Using Dried Blood Spot (DBS) Technology in Drug Discovery Wensheng Lang, Jenson Qi, and Gary W. Caldwell 28. In Vitro Trapping and Screening of Reactive Metabolites Using Liquid Chromatography-Mass Spectrometry Zhengyin Yan and Gary W. Caldwell 29. Quantitative Assessment of Reactive Metabolites Jie Chen, Rongfang Fran Xu, Wing W. Lam, Jose Silva, and Heng Keang Lim 30. In Vitro Assessment of the Reactivity of Acyl Glucuronides Rongfang Fran Xu, Wing W. Lam, Jie Chen, Michael McMillian, Jose Silva, and Heng Keang Lim 31. In Vitro COMET Assay for Testing Genotoxicity of Chemicals Haixia Lin, Nan Mei, and Mugimane G. Manjanatha 32. Assessing DNA Damage Using a Reporter Gene System Michael Biss and Wei Xiao 33. Improved AMES Test for Genotoxicity Assessment of Drugs: Preincubation Assay Using a Low Concentration of Dimethyl Sulfoxide Atsushi Hakura 34. Methods for Using the Mouse Lymphoma Assay to Screen for Chemical Mutagenicity and Photo-Mutagenicity Nan Mei, Xiaoqing Guo, and Martha M. Moore

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