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019 _a904539318
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020 _a9781118788493
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020 _a1118788524
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020 _a9781322572406
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020 _a1322572402
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020 _z9781118788356
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020 _z1118788354
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035 _a(OCoLC)893389733
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_z(OCoLC)960204304
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082 0 0 _a615.7/8
_223
049 _aMAIN
245 0 0 _aBlood-brain barrier in drug discovery :
_boptimizing brain exposure of CNS drugs and minimizing brain side effects for peripheral drugs /
_cedited by Li Di, Edward H. Kerns.
246 3 0 _aOptimizing brain exposure of CNS drugs and minimizing brain side effects for peripheral drugs
264 1 _aHoboken, New Jersey :
_bWiley,
_c[2015]
264 4 _c©2015
300 _a1 online resource (xiv, 586 pages, 4 unnumbered pages of plates) :
_billustrations (some color)
336 _atext
_btxt
_2rdacontent
336 _astill image
_bsti
_2rdacontent
337 _acomputer
_bc
_2rdamedia
338 _aonline resource
_bcr
_2rdacarrier
504 _aIncludes bibliographical references and index.
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.
588 _aDescription based on online resource; title from PDF title page (ebrary, viewed May 9, 2016).
505 0 _aIntroduction and overview / Li Di, and Edward H. Kerns -- Part 1: Pharmacokinetics of brain exposure. Pharmacokinetics of CNS penetration / Andreas Reichel -- Free drug hypothesis for CNS drug candidates / Xingrong Liu and Cuiping Chen -- Species differences and impact of disease state on BBB / Jean-Marie Nicolas -- Part 2: Mechanisms of drugs across the blood-brain barrier. Passive diffusion permeability of the BBB: examples and SAR / Scott Summerfield, Phil Jeffrey, Jasminder Sahi, and Liangfu Chen -- Efflux transport at the BBB: examples and SAR / Jerome Hochman -- Establishment of P-glycoprotein structure-transport relationships to optimize CNS exposure in drug discovery / Jerome H. Hochman, Sookhee N. Ha, and Robert P. Sheridan -- Uptake transport at the BBB: examples and SAR / Ziquiang Cheng and Qian Liu -- Transport of protein and antibody therapeutics across the blood-brain barrier / William M. Pardridge -- Part 3: Predicting and measuring brain exposure of drugs. In silico tools for assessing brain exposure / Hongming Chen, Susanne Winiwarter, and Ola Engkvist -- In vitro assays for assessing BBB permeability: vascular cells, artificial membranes, brain slice, cell uptake / Alex Avdeef, Mária A. Deli, and Winfried Neuhaus -- Human-based in vitro endothelial cell models / Hannah K. Wilson and Eric Shusta -- Methods for assessing brain binding / Li Di and Cheng Chang -- In vivo studies of brain exposure in drug discovery / Edward H. Kerns -- PBPK modelling approach for predictions of human CNS drug brain distribution / Elizabeth C.M. de Lange -- PK/PD modeling of CNS drug candidates / Johan Gabrielsson, Stephan Hjorth, and Lambertus A. Peletier -- Microdialysis to assess free drug concentration in brain / William Kielbasa and Robert E. Stratford, Jr. -- Imaging techniques for central nervous system (CNS) drug discovery / Lei Zhang and Anabella Villalobos -- Part 4: Modulating brain penetration of leads during drug discovery. Designing CNS drugs for optimal brain exposure / Zoran Rankovic -- Case studies of CNS drug optimization: medicinal chemistry and CNS biology perspectives / Kevin J. Hodgetts -- Designing peripheral drugs for minimal brain exposure / Peter Bungay, Sharan Bagal, and Andy Pike -- Case studies of non-CNS drugs to minimize brain penetration: nonsedative antihistamines / Andrew Crowe -- Part 5: Case studies in CNS drug discovery. Case study 1: the discovery and development of perampanel / Antonio Laurenza, Jim Ferry, Haichen Yang, Shigeki Hibi, Takahisa Hanada, and Andrew Satlin -- Case study 2: the discovery and development of the multimodal acting antidepressant vortioxetine / Christoffer Bundgaard, Alan L. Pehrson, Connie Sánchez, and Benny Bang-Andersen -- Part 6: Drug delivery techniques to CNS. Brain delivery using nanotechnology / Huile Gao and Xinguo Jiang -- Intranasal delivery to the central nervous system / Lisbeth Illum -- Part 7: Future prospects in blood-brain barrier understanding and drug discovery. Future perspectives / N. Joan Abbott .
650 0 _aBlood-brain barrier
_xMetabolism.
650 0 _aDrug development.
650 7 _aMEDICAL
_xPharmacology.
_2bisacsh
650 1 2 _aBlood-Brain Barrier
_xmetabolism.
650 1 2 _aCentral Nervous System Agents
_xpharmacokinetics.
650 2 2 _aBlood-Brain Barrier
_xdrug effects.
650 2 2 _aCentral Nervous System Diseases
_xdrug therapy.
650 2 2 _aDrug Discovery
_xmethods.
650 2 2 _aDrug-Related Side Effects and Adverse Reactions
_xprevention & control.
655 4 _aElectronic books.
655 0 _aElectronic books.
700 1 _aDi, Li,
_eeditor.
700 1 _aKerns, Edward Harvel,
_eeditor.
776 0 8 _iPrint version:
_tBlood-brain barrier in drug discovery.
_dHoboken, New Jersey : John Wiley & Sons Inc., [2015]
_z9781118788356
_w(DLC) 2014040935
_w(OCoLC)889736023
856 4 0 _uhttp://onlinelibrary.wiley.com/book/10.1002/9781118788523
_zWiley Online Library [Free Download only for SUST IP]
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