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020 _a9781592598007
024 7 _a10.1385/1592598005
_2doi
040 _aES-MaUEC
_bspa
_cES-MaUEC
_dES-MaUEC
050 4 _aRS407
_b2004 EB
245 0 0 _aOptimization in Drug Discovery
_cedited by Zhengyin Yan, Gary W. Caldwell
250 _a1st edition 2004
264 1 _aTotowa, NJ
_bHumana Press
_c2004
300 _a1 recurso en línea (XVI, 420 páginas)
336 _atexto
_btxt
_2rdacontent
337 _aelectrónico
_bc
_2rdamedia
338 _arecurso electrónico
_bcr
_2rdacarrier
347 _aarchivo de texto
_bPDF
490 0 _aMethods in Pharmacology and Toxicology
_x1940-6053
505 0 _apKa, Solubility, and Lipophilicity -- Use of Caco-2 Cell Monolayers to Study Drug Absorption and Metabolism -- Absorption Screening Using the PAMPA Approach -- In Situ Single-Pass Perfused Rat Intestinal Model for Absorption and Metabolism -- In Vitro Permeation Study With Bovine Brain Microvessel Endothelial Cells -- An Enzymatic Microplate Assay for Testing P-Glycoprotein Substrates and Inhibitors -- Evaluation of Drug-Transporter Interactions Using In Vitro Cell Models -- Plasma Protein-Binding Methods in Drug Discovery -- Isothermal Titration Calorimetry Characterization of Drug-Binding Energetics to Blood Proteins -- Metabolic Stability Assessed by Liver Microsomes and Hepatocytes -- In Vitro Drug Metabolite Profiling Using Hepatic S9 and Human Liver Microsomes -- In Vitro Identification of UDP-Glucuronosyltransferases (UGTs) Involved in Drug Metabolism -- In Vitro CYP Induction in Human Hepatocytes -- High-Throughput Screening of Human Cytochrome P450 Inhibitors Using Fluorometric Substrates -- Evaluation of Cytochrome P450 Inhibition in Human Liver Microsomes -- Identification of CYP Mechanism-Based Inhibitors -- Detection of DNA Adducts by 32P-Postlabeling Analysis -- Covalent DNA Adduct Formation Mediated by Cytochrome P450 -- Application of In Vitro Comet Assay for Genotoxicity Testing -- Assessing DNA Damage Using a Reporter Gene System -- Improvement of the Ames Test Using Human Liver S9 Preparation -- Screening for Chemical Mutagens Using the Mouse Lymphoma Assay -- A High-Throughput Binding Assay for HERG -- In Vitro Drug Metabolism -- In Vitro Screening Assay of the Reactivity of Acyl Glucuronides.
520 _aAlthough parallel synthesis combined with high-throughput screening has made it easier to generate highly potent drug candidates, many of these compounds never make the grade because they either prove to be unsafe or lack the necessary physicochemical and pharmacokinetic properties. In Optimization in Drug Discovery: In Vitro Methods, a panel of researchers and experts from leading universities and major pharmaceutical companies from all over the world provide proven solutions to this expensive problem with a collection of cutting-edge experimental protocols for early in vitro evaluation of new chemical entities (NCE). These readily reproducible assays measure such critical parameters as physicochemical properties, adsorption, plasma binding, metabolism, drug interactions, and toxicity. All protocols follow the successful Methods in Molecular Biology™ series format, each one offering step-by-step laboratory instructions, an introduction outlining the principle behind the technique, lists of equipment and reagents, and tips on troubleshooting and avoiding known pitfalls. Comprehensive and highly practical, Optimization in Drug Discovery: In Vitro Methods systematically collects and describes the key methods for uncovering-as early in the discovery stage as possible-those defects that can eliminate candidate drugs from preclinical and clinical development.
988 _aSpringer_Protocols_2004
650 7 _2embne
_9141808
_aQuímica farmacéutica
776 0 8 _iPrinted edition:
_z9781617374999
776 0 8 _iPrinted edition:
_z9781588293329
776 0 8 _iPrinted edition:
_z9781489939449
856 4 0 _uhttps://go.openathens.net/redirector/universidadeuropea.es?url=https://doi.org/10.1385/1592598005
_zAcceso a este recurso digital (usuarios Universidad Europea de Madrid)
942 _2lcc
_cLE
998 _b10/2023
_dz
_ean
_zSI