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Blood-Brain Barrier in Drug Discovery

Blood-Brain Barrier in Drug Discovery
Author: Li Di
Publisher: John Wiley & Sons
Total Pages: 604
Release: 2015-02-02
Genre: Medical
ISBN: 1118788354

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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


Blood-Brain Barrier in Drug Discovery

Blood-Brain Barrier in Drug Discovery
Author: Li Di
Publisher: John Wiley & Sons
Total Pages: 600
Release: 2014-12-29
Genre: Medical
ISBN: 1118788540

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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 mostsignificant – and most challenging – areas of drugdiscovery. • Written by world experts to provide practicalsolutions to increase brain penetration or minimize CNSside-effects • Reviews state-of-the-art in silico, in vitro, and invivo tools to assess brain penetration and advanced CNS drugdelivery strategies • Covers BBB physiology, medicinal chemistry designprinciples, free drug hypothesis for the BBB, and transportmechanisms including passive diffusion, uptake/efflux transporters,and receptor-mediated processes • Highlights the advances in modelling BBBpharmacokinetics and dynamics relationships (PK/PD) andphysiologically-based pharmacokinetics (PBPK) • Discusses case studies of successful CNS and non-CNSdrugs, lessons learned and paths to the market


The Blood Brain Barrier (BBB)

The Blood Brain Barrier (BBB)
Author: Gert Fricker
Publisher: Springer
Total Pages: 169
Release: 2014-10-24
Genre: Science
ISBN: 3662437872

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Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors.


Brain Drug Targeting

Brain Drug Targeting
Author: William M. Pardridge
Publisher: Cambridge University Press
Total Pages: 377
Release: 2001-05-31
Genre: Medical
ISBN: 0521800773

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This challenging 2001 book reviews modern neurotherapeutics from the point of view of drug targeting.


Drug Transport Across the Blood-brain Barrier

Drug Transport Across the Blood-brain Barrier
Author: A.G. de Boer
Publisher: CRC Press
Total Pages: 240
Release: 1997-04-08
Genre: Medical
ISBN: 9789057020322

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The availability of various in vitro and in vivo techniques has considerably advanced the research on drug transport and metabolism across the blood-brain barrier (BBB). These specialized and sophisticated experimental strategies are of fundamental importance if one is to gain a greater understanding of enhanced and selective drug delivery to the brain. The reader will find in this book methods for in vitro endothelial/astrocyte cell culture models, and for in vivo intracerebral microdialysis to study drug tranport across the BBB. This book, however, is not merely a laboratory manual consisting of recipes for BBB research; it permits the presentation of the different methods in fine detail, revealing tricks and short cuts that frequently do not appear in the literature. The researcher is well aware that differences (subtle or otherwise) in experimental steps used in different laboratories may influence the outcome of any particular procedure. The book also illustrates the accessibility and the application of the different methods in different species. Background information of the protocol is given in every chapter, which also contains a literature list that the reader may wish to refer to for further information. This volume will be invaluable to basic researchers as well as to those involved in the search for agents suitable for pharmaceutic intervention in the central nervous system.


Drug-like Properties: Concepts, Structure Design and Methods

Drug-like Properties: Concepts, Structure Design and Methods
Author: Li Di
Publisher: Elsevier
Total Pages: 549
Release: 2010-07-26
Genre: Science
ISBN: 0080557619

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Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. Serves as an essential working handbook aimed at scientists and students in medicinal chemistry Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies Discusses improvements in pharmacokinetics from a practical chemist's standpoint


The Blood-brain Barrier and Drug Delivery of the CNS

The Blood-brain Barrier and Drug Delivery of the CNS
Author: Michael William Blackburn Bradbury
Publisher:
Total Pages: 264
Release: 2000
Genre: MEDICAL
ISBN: 9780367800529

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This timely and compact monograph addresses how to determine drug permeability across the blood-brain barrier more effectively. Focusing on the physiological mechanisms that influence the passage of agents into the brain, the book covers the latest research on the blood-brain barrier, the current problems of and solutions to drug delivery to the central nervous system (CNS), existing strategies, and prospects for future research.Avoid excessive in vivo experimentation and utilize timesaving in vitro techniques. A concise reference with reviews from nearly 40 international specialists in diverse fields, The Blood-Brain Barrier and Drug Delivery to the CNSassesses the properties of the blood-brain barrier to determine and measure drug permeability in animals and humans presents techniques to predict successful drug uptake through in vitro systems or by computation of physicochemical parameters examines the multidrug resistance protein P-glycoprotein as a natural transporter analyzes current drug designs to known requirements for transport looks at drug delivery systems for the brain and much more!Densely packed with over 800 literature references, drawings, photographs, x-rays, tables, and equations, The Blood-Brain Barrier and Drug Delivery to the CNS is a vital addition to the bookshelves of biochemists, pharmacists, clinical and research pharmacologists, neuroscientists and neurologists, and graduate and medical school students in these disciplines.


Drug Delivery to the Brain

Drug Delivery to the Brain
Author: Margareta Hammarlund-Udenaes
Publisher: Springer Science & Business Media
Total Pages: 737
Release: 2013-12-03
Genre: Medical
ISBN: 1461491053

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The development of new CNS drugs is notoriously difficult. Drugs must reach CNS target sites for action and these sites are protected by a number of barriers, the most important being the blood –brain barrier (BBB). Many factors are therefore critical to consider for CNS drug delivery, e.g. active/passive transport across the BBB, intra-brain distribution, and central/systemic pharmacokinetics, to name a few. Neurological disease and trauma conditions add further complexity because CNS barriers, drug distribution and pharmacokinetics are dynamic and often changed by disease/trauma. Knowledge of all these factors and their interplay in different conditions is of utmost importance for proper CNS drug development and disease treatment. In recent years much information has become available for a better understanding of the many factors important for CNS drug delivery and how they interact to affect drug action. This book describes small and large drug delivery to the brain with an emphasis on the physiology of the BBB and the principles and concepts for drug delivery across the BBB and distribution within the brain. It contains methods descriptions for studying drug delivery, routes and approaches of administering drugs into the brain, the influence of disease, and drug industry perspectives. Therewith, it contributes to an in-depth understanding of the interplay between brain (patho)-physiology and drug characteristics. Furthermore, the content is designed to be both cutting-edge and educational, so that the book can be used in high-level training of academic and industry scientists with full references to original publications. ​


The Blood-brain Barrier and Drug Delivery to the Cns

The Blood-brain Barrier and Drug Delivery to the Cns
Author: Michael Bradbury
Publisher: CRC Press
Total Pages: 264
Release: 2019-08-30
Genre:
ISBN: 9780367398668

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This timely and compact monograph addresses how to determine drug permeability across the blood-brain barrier more effectively. Focusing on the physiological mechanisms that influence the passage of agents into the brain, the book covers the latest research on the blood-brain barrier, the current problems of and solutions to drug delivery to the central nervous system (CNS), existing strategies, and prospects for future research. Avoid excessive in vivo experimentation and utilize timesaving in vitro techniques. A concise reference with reviews from nearly 40 international specialists in diverse fields, The Blood-Brain Barrier and Drug Delivery to the CNS assesses the properties of the blood-brain barrier to determine and measure drug permeability in animals and humans presents techniques to predict successful drug uptake through in vitro systems or by computation of physicochemical parameters examines the multidrug resistance protein P-glycoprotein as a natural transporter analyzes current drug designs to known requirements for transport looks at drug delivery systems for the brain and much more! Densely packed with over 800 literature references, drawings, photographs, x-rays, tables, and equations, The Blood-Brain Barrier and Drug Delivery to the CNS is a vital addition to the bookshelves of biochemists, pharmacists, clinical and research pharmacologists, neuroscientists and neurologists, and graduate and medical school students in these disciplines.


The ADME Encyclopedia

The ADME Encyclopedia
Author: Alan Talevi
Publisher: Springer Nature
Total Pages: 1209
Release: 2022-06-14
Genre: Medical
ISBN: 3030848604

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The ADME Encyclopedia covers pharmacokinetic phenomena (Absorption, Distribution, Metabolism and Excretion processes) and their relationship with the design of pharmaceutical carriers and the success of drug therapies. It covers both basic and advanced knowledge, serving as introductory material for students of biomedical careers and also as reference, updated material for graduates and professionals working in any field related to pharmaceutical sciences (medicine, pharmaceutical technology, materials science, medicinal chemistry). Structured as alphabetically ordered entries with cross-references, the Encyclopedia not only provides basic knowledge on ADME processes, but also detailed entries on some advanced subjects such as drug transporters, last generation pharmaceutical carriers, pharmacogenomics, personalized medicine, bioequivalence studies, biowaivers, biopharmaceuticals, gene delivery, pharmacometrics, pharmacokinetic drug interactions or in silico and in vitro assessment of ADME properties