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Titlebook: Optimization in Drug Discovery; Zhengyin Yan,Gary W. Caldwell Book 2004 Humana Press 2004

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Zhengyin Yan,Gary W. CaldwellIncludes supplementary material:
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Optimization in Drug Discovery978-1-59259-800-7Series ISSN 1557-2153 Series E-ISSN 1940-6053
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Absorption Screening Using the PAMPA Approach,s chapter also discusses how PAMPA has relevance in preformulation research. A detailed PAMPA protocol is presented, with step-by-step instructions for a popular version of the assay, using relatively inexpensive and readily obtainable components.
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An Enzymatic Microplate Assay for Testing P-Glycoprotein Substrates and Inhibitors,erapamil, vinblastine, and progesterone) in addition to its basal ATPase activity. This assay uses a coupled enzyme system with spectrophotometric detection for measurement on P-gp-containing native membrane vesicles. This assay may be performed on 96- or 384-well microplates and is therefore suitable for high-throughput screenings.
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In Vitro CYP Induction in Human Hepatocytes, nontransplantable human liver followed by their culture and treatment with new chemical entities and/or known inducers of cytochrome P450. Enzyme induction in cultured human hepatocytes can be assessed by measuring the levels of messenger ribonucleic acid, immunoreactive protein, and/or cytochrome P450 enzyme activity as outlined in this chapter.
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