Blood-brain barrier in drug discovery : optimizing brain exposure of CNS drugs and minimizing brain side effects for peripheral drugs /

• Άλλοι συγγραφείς: Di, Li (Επιμελητής έκδοσης), Kerns, Edward Harvel (Επιμελητής έκδοσης)
• Μορφή: Ηλ. βιβλίο
• Γλώσσα: English
• Έκδοση: Hoboken, New Jersey : Wiley, [2015]
• Θέματα: Blood-brain barrier > Metabolism.; Drug development.; MEDICAL > Pharmacology.; Blood-Brain Barrier > metabolism.; Central Nervous System Agents > pharmacokinetics.; Blood-Brain Barrier > drug effects.; Central Nervous System Diseases > drug therapy.; Drug Discovery > methods.; Drug-Related Side Effects and Adverse Reactions > prevention & control.; Electronic books.

"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...

Πίνακας περιεχομένων:

• Introduction 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 .