Drug-like Properties: Concepts, Structure Design and Methods

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Author :
Publisher : Elsevier
ISBN 13 : 0080557619
Total Pages : 549 pages
Book Rating : 4.0/5 (85 download)

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Book Synopsis Drug-like Properties: Concepts, Structure Design and Methods by : Li Di

Download or read book Drug-like Properties: Concepts, Structure Design and Methods written by Li Di and published by Elsevier. This book was released on 2010-07-26 with total page 549 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Planaria: A Model for Drug Action and Abuse

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Author :
Publisher : CRC Press
ISBN 13 : 1498713599
Total Pages : 150 pages
Book Rating : 4.4/5 (987 download)

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Book Synopsis Planaria: A Model for Drug Action and Abuse by : Robert B. Raffa

Download or read book Planaria: A Model for Drug Action and Abuse written by Robert B. Raffa and published by CRC Press. This book was released on 2008-12-03 with total page 150 pages. Available in PDF, EPUB and Kindle. Book excerpt: The study of drug action has benefitted greatly from the development and use of in vivo model systems. In model systems, manipulations and observations can be more rigorously controlled and screens of novel therapeutic agents can be more safely conducted.No single model system provides all of the possible advantages. At one end, mammalian models al

Sites of Drug Action in the Human Brain

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Publisher : CRC Press
ISBN 13 : 9780849376535
Total Pages : 202 pages
Book Rating : 4.3/5 (765 download)

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Book Synopsis Sites of Drug Action in the Human Brain by : Anat Biegon

Download or read book Sites of Drug Action in the Human Brain written by Anat Biegon and published by CRC Press. This book was released on 1995-02-24 with total page 202 pages. Available in PDF, EPUB and Kindle. Book excerpt: Sites of Drug Action in the Human Brain uses the results of recent analyses of the regional brain distribution and binding pattern of drugs in the human brain. This new book specifically addresses drugs of abuse and treats the effects of various drugs on behavior and mood, as well as on metabolism and blood flow in the human brain. It also presents the methodological aspects of investigating the sites of drug action in the human brain. Because it focuses on the living human brain, this book differs from other books on the subject, which primarily use the results of postmortem studies. Sites of Drug Action in the Human Brain therefore provides valuable information on the clinical aspects of drug intoxification, addiction, and toxicity.

Drug Transporters

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Publisher : Springer Science & Business Media
ISBN 13 : 3642145418
Total Pages : 457 pages
Book Rating : 4.6/5 (421 download)

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Book Synopsis Drug Transporters by : Martin F. Fromm

Download or read book Drug Transporters written by Martin F. Fromm and published by Springer Science & Business Media. This book was released on 2010-11-19 with total page 457 pages. Available in PDF, EPUB and Kindle. Book excerpt: It is increasingly recognized that various transporter proteins are expressed throughout the body and determine absorption, tissue distribution, biliary and renal elimination of endogenous compounds and drugs and drug effects. This book will give an overview on the transporter families which are most important for drug therapy. Most chapters will focus on one transporter family highlighting tissue expression, substrates, inhibitors, knock-out mouse models and clinical studies.

Improving and Accelerating Therapeutic Development for Nervous System Disorders

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Publisher : National Academies Press
ISBN 13 : 0309292492
Total Pages : 107 pages
Book Rating : 4.3/5 (92 download)

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Book Synopsis Improving and Accelerating Therapeutic Development for Nervous System Disorders by : Institute of Medicine

Download or read book Improving and Accelerating Therapeutic Development for Nervous System Disorders written by Institute of Medicine and published by National Academies Press. This book was released on 2014-02-06 with total page 107 pages. Available in PDF, EPUB and Kindle. Book excerpt: Improving and Accelerating Therapeutic Development for Nervous System Disorders is the summary of a workshop convened by the IOM Forum on Neuroscience and Nervous System Disorders to examine opportunities to accelerate early phases of drug development for nervous system drug discovery. Workshop participants discussed challenges in neuroscience research for enabling faster entry of potential treatments into first-in-human trials, explored how new and emerging tools and technologies may improve the efficiency of research, and considered mechanisms to facilitate a more effective and efficient development pipeline. There are several challenges to the current drug development pipeline for nervous system disorders. The fundamental etiology and pathophysiology of many nervous system disorders are unknown and the brain is inaccessible to study, making it difficult to develop accurate models. Patient heterogeneity is high, disease pathology can occur years to decades before becoming clinically apparent, and diagnostic and treatment biomarkers are lacking. In addition, the lack of validated targets, limitations related to the predictive validity of animal models - the extent to which the model predicts clinical efficacy - and regulatory barriers can also impede translation and drug development for nervous system disorders. Improving and Accelerating Therapeutic Development for Nervous System Disorders identifies avenues for moving directly from cellular models to human trials, minimizing the need for animal models to test efficacy, and discusses the potential benefits and risks of such an approach. This report is a timely discussion of opportunities to improve early drug development with a focus toward preclinical trials.

Principles of Safety Pharmacology

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Publisher : Springer
ISBN 13 : 366246943X
Total Pages : 477 pages
Book Rating : 4.6/5 (624 download)

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Book Synopsis Principles of Safety Pharmacology by : Michael K. Pugsley

Download or read book Principles of Safety Pharmacology written by Michael K. Pugsley and published by Springer. This book was released on 2015-06-19 with total page 477 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book illustrates, in a comprehensive manner, the most current areas of importance to Safety Pharmacology, a burgeoning unique pharmacological discipline with important ties to academia, industry and regulatory authorities. It provides readers with a definitive collection of topics containing essential information on the latest industry guidelines and overviews current and breakthrough topics in both functional and molecular pharmacology. An additional novelty of the book is that it constitutes academic, pharmaceutical and biotechnology perspectives for Safety Pharmacology issues. Each chapter is written by an expert in the area and includes not only a fundamental background regarding the topic but also detailed descriptions of currently accepted, validated models and methods as well as innovative methodologies used in drug discovery.

Anesthetic Pharmacology

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Publisher : Cambridge University Press
ISBN 13 : 1139497022
Total Pages : 2902 pages
Book Rating : 4.1/5 (394 download)

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Book Synopsis Anesthetic Pharmacology by : Alex S. Evers

Download or read book Anesthetic Pharmacology written by Alex S. Evers and published by Cambridge University Press. This book was released on 2011-03-10 with total page 2902 pages. Available in PDF, EPUB and Kindle. Book excerpt: In recent years our understanding of molecular mechanisms of drug action and interindividual variability in drug response has grown enormously. Meanwhile, the practice of anesthesiology has expanded to the preoperative environment and numerous locations outside the OR. Anesthetic Pharmacology: Basic Principles and Clinical Practice, 2nd edition, is an outstanding therapeutic resource in anesthesia and critical care: Section 1 introduces the principles of drug action, Section 2 presents the molecular, cellular and integrated physiology of the target organ/functional system and Section 3 reviews the pharmacology and toxicology of anesthetic drugs. The new Section 4, Therapeutics of Clinical Practice, provides integrated and comparative pharmacology and the practical application of drugs in daily clinical practice. Edited by three highly acclaimed academic anesthetic pharmacologists, with contributions from an international team of experts, and illustrated in full colour, this is a sophisticated, user-friendly resource for all practitioners providing care in the perioperative period.

Mechanisms of Drug Toxicity

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Publisher : Elsevier
ISBN 13 : 1483157202
Total Pages : 113 pages
Book Rating : 4.4/5 (831 download)

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Book Synopsis Mechanisms of Drug Toxicity by : H. Rašková

Download or read book Mechanisms of Drug Toxicity written by H. Rašková and published by Elsevier. This book was released on 2013-10-22 with total page 113 pages. Available in PDF, EPUB and Kindle. Book excerpt: Mechanisms of Drug Toxicity, Volume 4 presents the proceedings of the 3rd International Pharmacological Meeting held in Sao Paulo, Brazil in 1966. The book discusses the drug-induced pathobiotic effects; the mechanisms of adverse reactions; and enzyme induction in the mechanism of chronic toxicity. The text also describes the influence of inducing substances on the growth of liver and microsomal electron transport systems; the quantitative aspects of chronic toxicity; and the facts and fallacies in predicting drug effects in human.

The Prevention and Treatment of Missing Data in Clinical Trials

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Publisher : National Academies Press
ISBN 13 : 030918651X
Total Pages : 163 pages
Book Rating : 4.3/5 (91 download)

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Book Synopsis The Prevention and Treatment of Missing Data in Clinical Trials by : National Research Council

Download or read book The Prevention and Treatment of Missing Data in Clinical Trials written by National Research Council and published by National Academies Press. This book was released on 2010-12-21 with total page 163 pages. Available in PDF, EPUB and Kindle. Book excerpt: Randomized clinical trials are the primary tool for evaluating new medical interventions. Randomization provides for a fair comparison between treatment and control groups, balancing out, on average, distributions of known and unknown factors among the participants. Unfortunately, these studies often lack a substantial percentage of data. This missing data reduces the benefit provided by the randomization and introduces potential biases in the comparison of the treatment groups. Missing data can arise for a variety of reasons, including the inability or unwillingness of participants to meet appointments for evaluation. And in some studies, some or all of data collection ceases when participants discontinue study treatment. Existing guidelines for the design and conduct of clinical trials, and the analysis of the resulting data, provide only limited advice on how to handle missing data. Thus, approaches to the analysis of data with an appreciable amount of missing values tend to be ad hoc and variable. The Prevention and Treatment of Missing Data in Clinical Trials concludes that a more principled approach to design and analysis in the presence of missing data is both needed and possible. Such an approach needs to focus on two critical elements: (1) careful design and conduct to limit the amount and impact of missing data and (2) analysis that makes full use of information on all randomized participants and is based on careful attention to the assumptions about the nature of the missing data underlying estimates of treatment effects. In addition to the highest priority recommendations, the book offers more detailed recommendations on the conduct of clinical trials and techniques for analysis of trial data.

Thermodynamics and Kinetics of Drug Binding

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Publisher : John Wiley & Sons
ISBN 13 : 352733582X
Total Pages : 360 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Thermodynamics and Kinetics of Drug Binding by : György Keserü

Download or read book Thermodynamics and Kinetics of Drug Binding written by György Keserü and published by John Wiley & Sons. This book was released on 2015-08-17 with total page 360 pages. Available in PDF, EPUB and Kindle. Book excerpt: This practical reference for medicinal and pharmaceutical chemists combines the theoretical background with modern methods as well as applications from recent lead finding and optimization projects. Divided into two parts on the thermodynamics and kinetics of drug-receptor interaction, the text provides the conceptual and methodological basis for characterizing binding mechanisms for drugs and other bioactive molecules. It covers all currently used methods, from experimental approaches, such as ITC or SPR, right up to the latest computational methods. Case studies of real-life lead or drug development projects are also included so readers can apply the methods learned to their own projects. Finally, the benefits of a thorough binding mode analysis for any drug development project are summarized in an outlook chapter written by the editors.

Pharmacokinetics and Pharmacodynamics of Biotech Drugs

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Publisher : John Wiley & Sons
ISBN 13 : 3527609520
Total Pages : 426 pages
Book Rating : 4.5/5 (276 download)

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Book Synopsis Pharmacokinetics and Pharmacodynamics of Biotech Drugs by : Bernd Meibohm

Download or read book Pharmacokinetics and Pharmacodynamics of Biotech Drugs written by Bernd Meibohm and published by John Wiley & Sons. This book was released on 2006-12-13 with total page 426 pages. Available in PDF, EPUB and Kindle. Book excerpt: This first ever coverage of the pharmacokinetic and pharmacodynamic characteristics of biopharmaceuticals meets the need for a comprehensive book in this field. It spans all topics from lead identification right up to final-stage clinical trials. Following an introduction to the role of PK and PD in the development of biotech drugs, the book goes on to cover the basics, including the pharmacokinetics of peptides, monoclonal antibodies, antisense oligonucleotides, as well as viral and non-viral gene delivery vectors. The second section discusses such challenges and opportunities as pulmonary delivery of proteins and peptides, and the delivery of oligonucleotides. The final section considers the integration of PK and PD concepts into the biotech drug development plan, taking as case studies the preclinical and clinical drug development of tasidotin, as well as the examples of cetuximab and pegfilgrastim. The result is vital reading for all pharmaceutical researchers.

An Essay Concerning Human Understanding

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Publisher :
ISBN 13 :
Total Pages : 438 pages
Book Rating : 4.:/5 (2 download)

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Book Synopsis An Essay Concerning Human Understanding by : John Locke

Download or read book An Essay Concerning Human Understanding written by John Locke and published by . This book was released on 1924 with total page 438 pages. Available in PDF, EPUB and Kindle. Book excerpt: First published in 1690, John Locke (1632-1704) provides an account of how we acquire everyday, mathematical, natural scientific, religious and ethical knowledge. Rejecting the theory that some knowledge is innate, he argues that it derives from sense perceptions and experience, as analysed and developed by reason. While defending these central claims with vigorous common sense, he offers many incidental reflections on space and time, meaning, free will and personal identity.

Caffeine for the Sustainment of Mental Task Performance

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Publisher : National Academies Press
ISBN 13 : 0309082587
Total Pages : 172 pages
Book Rating : 4.3/5 (9 download)

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Book Synopsis Caffeine for the Sustainment of Mental Task Performance by : Institute of Medicine

Download or read book Caffeine for the Sustainment of Mental Task Performance written by Institute of Medicine and published by National Academies Press. This book was released on 2002-01-07 with total page 172 pages. Available in PDF, EPUB and Kindle. Book excerpt: This report from the Committee on Military Nutrition Research reviews the history of caffeine usage, the metabolism of caffeine, and its physiological effects. The effects of caffeine on physical performance, cognitive function and alertness, and alleviation of sleep deprivation impairments are discussed in light of recent scientific literature. The impact of caffeine consumption on various aspects of health, including cardiovascular disease, reproduction, bone mineral density, and fluid homeostasis are reviewed. The behavioral effects of caffeine are also discussed, including the effect of caffeine on reaction to stress, withdrawal effects, and detrimental effects of high intakes. The amounts of caffeine found to enhance vigilance and reaction time consistently are reviewed and recommendations are made with respect to amounts of caffeine appropriate for maintaining alertness of military personnel during field operations. Recommendations are also provided on the need for appropriate labeling of caffeine-containing supplements, and education of military personnel on the use of these supplements. A brief review of some alternatives to caffeine is also provided.

A Pharmacology Primer

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Publisher : Academic Press
ISBN 13 : 0128139587
Total Pages : 489 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis A Pharmacology Primer by : Terry P. Kenakin

Download or read book A Pharmacology Primer written by Terry P. Kenakin and published by Academic Press. This book was released on 2018-10-26 with total page 489 pages. Available in PDF, EPUB and Kindle. Book excerpt: A Pharmacology Primer: Techniques for More Effective and Strategic Drug Discovery, Fifth Edition features the latest ideas and research regarding the application of pharmacology to the process of drug discovery. Written by well-respected pharmacologist, Terry P. Kenakin, this primer is an indispensable resource for all those involved in drug discovery. This updated edition has been thoroughly revised to include material on quantifying drug efficacy through bias and cluster analysis, the impact of molecular dynamics and protein structural analysis, the real time kinetic analysis of drug effect, virtual screening for new drug chemical scaffolds, and much more. With full color illustrations and new examples throughout, this book remains a top reference for all industry and academic scientists that is also ideal for students directly involved in drug discovery or pharmacologic research. - Highlights changes surrounding strategies for drug discovery, providing a comprehensive reference and featuring advances in the methods involved - Includes multiple new sections, such as development and utilization of models in pharmacology, de-orphanization of new drug targets, predicting impact of disease on drug pharmacokinetics, and the impact of enzyme kinetics on drug-drug interactions - Illustrates the application of rapid inexpensive assays to predict activity in the therapeutic setting, showing data outcomes and the limitations inherent in interpreting this data

Adverse Effects of Engineered Nanomaterials

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Publisher : Academic Press
ISBN 13 : 0123869404
Total Pages : 367 pages
Book Rating : 4.1/5 (238 download)

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Book Synopsis Adverse Effects of Engineered Nanomaterials by : Bengt Fadeel

Download or read book Adverse Effects of Engineered Nanomaterials written by Bengt Fadeel and published by Academic Press. This book was released on 2012-01-27 with total page 367 pages. Available in PDF, EPUB and Kindle. Book excerpt: An essential reference that discusses occupational exposure and the adverse health effects of engineered nanomaterials and highlights current and future biomedical applications of these nanomaterials in relation to nanosafety.

Fundamentals of Antimicrobial Pharmacokinetics and Pharmacodynamics

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Publisher : Springer Science & Business Media
ISBN 13 : 0387756132
Total Pages : 467 pages
Book Rating : 4.3/5 (877 download)

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Book Synopsis Fundamentals of Antimicrobial Pharmacokinetics and Pharmacodynamics by : Alexander A. Vinks

Download or read book Fundamentals of Antimicrobial Pharmacokinetics and Pharmacodynamics written by Alexander A. Vinks and published by Springer Science & Business Media. This book was released on 2013-11-23 with total page 467 pages. Available in PDF, EPUB and Kindle. Book excerpt: Over the past decade, significant progress has been made in the theory and applications of pharmacodynamics of antimicrobial agents. On the basis of pharmacokinetic-pharmacodynamic modeling concepts it has become possible to describe and predict the time course of antimicrobial effects under normal and pathophysiological conditions. The study of pharmacokinetic-pharmacodynamic relationships can be of considerable value in understanding drug action, defining optimal dosing regimens, and in making predictions under new or changing pre-clinical and clinical circumstances. Not surprisingly, pharmacokinetic-pharmacodynamic modeling concepts are increasingly applied in both basic and clinical research as well as in drug development. The book will be designed as a reference on the application of pharmacokinetic-pharmacodynamic principles for the optimization of antimicrobial therapy, namely pharmacotherapy, and infectious diseases. The reader will be introduced to various aspects of the fundamentals of antimicrobial pharmacodynamics, the integration of pharmacokinetics with pharmacodynamics for all major classes of antibiotics, and the translation of in vitro and animal model data to basic research and clinical situations in humans.

Oxidative Stress and Neurodegenerative Disorders

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Publisher : Elsevier
ISBN 13 : 0080489494
Total Pages : 795 pages
Book Rating : 4.0/5 (84 download)

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Book Synopsis Oxidative Stress and Neurodegenerative Disorders by : G. Ali Qureshi

Download or read book Oxidative Stress and Neurodegenerative Disorders written by G. Ali Qureshi and published by Elsevier. This book was released on 2007-03-22 with total page 795 pages. Available in PDF, EPUB and Kindle. Book excerpt: Oxidative stress is the result of an imbalance in pro-oxidant/antioxidant homeostasis that leads to the generation of toxic reactive oxygen species. Brain cells are continuously exposed to reactive oxygen species generated by oxidative metabolism, and in certain pathological conditions defense mechanisms against oxygen radicals may be weakened and/or overwhelmed. DNA is a potential target for oxidative damage, and genomic damage can contribute to neuropathogenesis. It is important therefore to identify tools for the quantitative analysis of DNA damage in models on neurological disorders. This book presents detailed information on various neurodegenerative disorders and their connection with oxidative stress. This information will provide clinicians with directions to treat these disorders with appropriate therapy and is also of vital importance for the drug industries for the design of new drugs for treatment of degenerative disorders.* Contains the latest information on the subject of neurodegenerative disorders* Reflects on various factors involved in degeneration and gives suggestions for how to tackle these problems