000744192 000__ 05384cam\a2200409\i\4500 000744192 001__ 744192 000744192 005__ 20210515112345.0 000744192 006__ m\\\\\o\\d\\\\\\\\ 000744192 007__ cr\cn\nnnunnun 000744192 008__ 141015t20152015njuad\\\ob\\\\001\0\eng\d 000744192 020__ $$z9781118788356 000744192 020__ $$a9781118788547$$qelectronic book 000744192 035__ $$a(CaPaEBR)ebr11005763 000744192 035__ $$a(OCoLC)893389733 000744192 040__ $$aCaPaEBR$$beng$$erda$$epn$$cCaPaEBR 000744192 05014 $$aRM315$$b.B56 2015eb 000744192 08204 $$a615.7/8$$223 000744192 24500 $$aBlood-brain barrier in drug discovery$$h[electronic resource] :$$boptimizing brain exposure of CNS drugs and minimizing brain side effects for peripheral drugs /$$cedited by Li Di, Edward H. Kerns. 000744192 264_1 $$aHoboken, New Jersey :$$bJohn Wiley & Sons Inc.,$$c[2015] 000744192 264_4 $$c©2015 000744192 300__ $$a1 online resource (607 pages) :$$billustrations. 000744192 336__ $$atext$$2rdacontent 000744192 337__ $$acomputer$$2rdamedia 000744192 338__ $$aonline resource$$2rdacarrier 000744192 504__ $$aIncludes bibliographical references and index. 000744192 5058_ $$aMachine generated contents note: Summary List of Chapters1. Overview/Introduction / Li Di (Pfizer Inc.), Edward H. Kerns (Pharmacokinetics of Brain Exposure)2. Pharmacokinetics of CNS penetration / Andreas Reichel (Bayer)3. Free Drug Hyposthesis for CNS Drug Candidates / Xingrong Liu (Genentech)4. Species Differences and impact of desease state on BBB / Jean-Marie Nicolas (UCB Pharma S.A.)Mechanisms of Drugs Across the Blood-Brain Barrier5. Passive diffusion permeability of the BBB - examples and SAR / Phil Jeffrey (GSK)6. Efflux transport at the BBB - examples and SAR / Jerome Hochman (Merck)7. Uptake transport at the BBB - examples and SAR / Zack Cheng (AstraZeneca)8. Uptake of proteins and antibodies at the BBB / William Pardridge (UCLA)Predicting and Measuring Brain Exposure of Drugs9. In silico tools for assessing brain exposure / Hongming Chen (AstraZeneca)10. In vitro assays for assessing BBB permeability - vascular cells, artificial membranes, brain slice, cell uptake / Winfried Neuhaus (University of Vienna)11. Human-based in vitro endothelial cell models / Eric Shusta (University of Wisconsin)12. In vitro assays for assessing brain binding / Li Di (Pfizer)13. In vivo studies of brain exposure / Edward H. Kerns14. PBPK models for BBB / Elizabeth de Lange (Leiden University)15. PK/PD modeling of CNS drug candidates / Johan Gabrielsson (Swedish University)16. Microdialysis to assess free drug concentration in brain / William Kielbasa (Lilly)17. Imaging technique for CNS drug discovery / Lei Zhang (Pfizer Inc.)Modulating Brain Penetration of Leads During Drug Discovery18. Designing CNS drugs for optimal brain exposure / Zoran Rankovic (Lilly)19. Case studies of CNS drug optimization - medicinal chemistry and CNS biology perspectives / Kevin J. Hodgetts (Harvard NeuroDiscovery Center)20. Designing peripheral drugs for minimal brain exposue / Peter Bungay (Pfizer)21. Case studies of non-CNS drugs to minimize brain penetration - Nonsudative antihistamines / Andrew Crowe (Curtin University)Case Studies in CNS Drug Discovery22. Case study 1 on discovery of a successful CNS drug - Fycompa (AMPA Receptor Antagonist) / Andrew Satlin and Antonio Laurenza (Eisai)23. Case study 2 on discovery of a successful CNS drug - Vortioxetine (Serotonin Modulator and Stimulator) / Benny Bang-Andersen (Lundbeck)Drug Delivery Techniques to CNS24. Brain delivery using nanotechnology / Xinguo Jiang (Fudan University)25. Intranasal delivery to CNS / Lisbeth Illum (University of Nottingham)Future Prospective in Blood Brain Barrier Advancement26. Conclusion Remarks / Joan Abbott (King's College). 000744192 506__ $$aAccess limited to authorized users. 000744192 520__ $$a"Focused on central nervous system (CNS) drug discovery efforts, this book educates drug researchers about the blood-brain barrier (BBB) so they can affect important improvements in one of the most significant - and most challenging - areas of drug discovery. Written by world experts to provide practical solutions to increase brain penetration or minimize CNS side-effects. Reviews state-of-the-art in silico, in vitro, and in vivo tools to assess brain penetration and advanced CNS drug delivery strategies. Covers BBB physiology, medicinal chemistry design principles, free drug hypothesis for the BBB, and transport mechanisms including passive diffusion, uptake/efflux transporters, and receptor-mediated processes. Highlights the advances in modelling BBB pharmacokinetics and dynamics relationships (PK/PD) and physiologically-based pharmacokinetics (PBPK). Discusses case studies of successful CNS and non-CNS drugs, lessons learned and paths to the market"--Provided by publisher. 000744192 588__ $$aDescription based on print version record. 000744192 650_0 $$aBrain$$xEffect of drugs on. 000744192 650_0 $$aBlood-brain barrier. 000744192 7001_ $$aDi, Li,$$eeditor. 000744192 7001_ $$aKerns, Edward Harvel,$$eeditor. 000744192 77608 $$iPrint version:$$tBlood-brain barrier in drug discovery : optimizing brain exposure of CNS drugs and minimizing brain side effects for peripheral drugs.$$dHoboken, New Jersey : John Wiley & Sons Inc., [2015]$$z9781118788356$$w(DNLM)101643550$$w(DLC)11005763 000744192 852__ $$bebk 000744192 85640 $$3ProQuest Ebook Central Academic Complete$$uhttps://univsouthin.idm.oclc.org/login?url=http://site.ebrary.com/lib/usiricelib/Doc?id=11005763$$zOnline Access 000744192 909CO $$ooai:library.usi.edu:744192$$pGLOBAL_SET 000744192 980__ $$aEBOOK 000744192 980__ $$aBIB 000744192 982__ $$aEbook 000744192 983__ $$aOnline