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Pharmacologic Analysis Of Drug Receptor Interaction


Pharmacologic Analysis Of Drug Receptor Interaction
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Pharmacologic Analysis Of Drug Receptor Interaction


Pharmacologic Analysis Of Drug Receptor Interaction
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Author : Terrence P. Kenakin
language : en
Publisher: Raven Press (ID)
Release Date : 1993

Pharmacologic Analysis Of Drug Receptor Interaction written by Terrence P. Kenakin and has been published by Raven Press (ID) this book supported file pdf, txt, epub, kindle and other format this book has been release on 1993 with Medical categories.


A guide to quantitative drug-receptor pharmacology, this new edition aims to cover all receptor systems, whether derived from molecular biology or animal studies. Using existing data, it demonstrates how theoretical models facilitate drug development, and integrates theory with practice. This second edition aims to be a valuable resource for all researchers involved in the drug design and development process. Not only has the text been updated and revised, but reflecting the significant technical breakthroughs of recent years, it now more generally encompasses all receptor systems, whether derived from molecular biology or whole animal studies. These systems are examined within the framework of current drug receptor theories, particularly the receptor occupation theory, the operational model of drug action and the ternary complex model.



Affinity And Efficacy The Components Of Drug Receptor Interactions


Affinity And Efficacy The Components Of Drug Receptor Interactions
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Author : Frederick J Ehlert
language : en
Publisher: World Scientific
Release Date : 2014-11-13

Affinity And Efficacy The Components Of Drug Receptor Interactions written by Frederick J Ehlert and has been published by World Scientific this book supported file pdf, txt, epub, kindle and other format this book has been release on 2014-11-13 with Medical categories.


The interaction of a drug with a receptor generates a code of information having components of affinity and efficacy. How this information is translated into a response depends on the unique cells, tissue, organ or system in which the receptor resides. This book describes how to analyze various responses to estimate the affinity and efficacy components of the initial drug-receptor interaction. More specifically, it describes how to measure the affinity and efficacy of drugs through the analysis of single receptor activity, the activation state of a population of receptors, and responses downstream from receptor activation. More light is thrown on ligand-gated ion channels and G protein-coupled receptors in this book.The topics discussed include radioligand binding, estimation of agonist affinity and efficacy, competitive antagonism, inverse agonism, allosteric agonists and modulators, agonist bias, modulation of pathway selectivity, and the estimation of ligand affinity for active and inactive receptor states. The natural history and structure of ligand-gated ion channels, G proteins, and G protein-coupled receptors are also discussed.



Kinetics Of Drug Action


Kinetics Of Drug Action
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Author : J.M. van Rossum
language : en
Publisher: Springer Science & Business Media
Release Date : 2012-12-06

Kinetics Of Drug Action written by J.M. van Rossum and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012-12-06 with Medical categories.


Most drugs, toxins, hormones, and the like bring about their biologic actions by reacting with specific receptors somewhere in the body. Scientists working in all areas of biologic science have shown increasing interest in the analysis of drug-receptor interactions in the broadest sense. Studies of drugs (binding) to receptors in situ and to isolated and partly purified receptors are becoming common practice. The action of a drug in the body is, however, a kinetic event not only with respect to transport of drug molecules to the environment of the receptors, but also with respect to the drug-receptor interaction itself. Kinetics of Drug Action is an integrative approach to drug transport through the body, membrane transport toward the receptors, and the kinetics of drug receptor interaction. This volume is aimed at providing a critical and penetrating study of the problems relevant to the kinetics or drug action from drug dosage to the final response. It is felt that the critical surveys presented in this volume will contribute significantly to receptor study research in various biologic fields and to a better understanding of drug action. I would like to express my gratitude to our secretary Miss MARGOT JANSSEN for the extensive typing of manuscripts and to our laboratory assistant Miss COBY HURKMANS for her dedicated assistance in the correcting some of the manuscripts and preparating the index.



Receptor Based Drug Design


Receptor Based Drug Design
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Author : Paul Leff
language : en
Publisher: CRC Press
Release Date : 1998-04-10

Receptor Based Drug Design written by Paul Leff and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 1998-04-10 with Medical categories.


Employing a wide range of examples from G-protein-coupled receptors and ligand-gated ion channels, this detailed, single-source reference illustrates the principles of pharmacological analysis and receptor classification that are the basis of rational drug design. Explains the experimental and theoretical methods used to characterize interactions between ligands and receptors-providing the pharmacological information needed to solve treatment problems and facilitate the drug design process! Demonstrating the achievements of the receptor-based approach in therapeutics and indicating future directions, Receptor-Based Drug Design introduces novel computer-assisted strategies for the design of new agonists, antagonists, and inverse agonists for G-protein-coupled receptors shows how to assess agonist concentration-effect curve data discusses radioligand binding assays presents new in vitro multiarray assays for G-protein-coupled receptors explains the use of individual second messenger signaling responses in analyzing drug-receptor interactions examines the role of electrophysiology in finding new drugs and drug targets describes selectively acting b-adrenoceptor agonists and glucocorticoid steroids for asthma treatment outlines the rationale for using angiotensin receptor antagonists and more! Written by over 25 international authorities and containing nearly 1200 bibliographic citations, Receptor-Based Drug Design is a practical resource for pharmacologists, pharmacists, and pharmaceutical scientists; organic and medicinal chemists and biochemists; molecular biologists; biomedical researchers; and upper-level undergraduate and graduate students in these disciplines.



Textbook Of Receptor Pharmacology Third Edition


Textbook Of Receptor Pharmacology Third Edition
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Author : John C. Foreman
language : en
Publisher: CRC Press
Release Date : 2011-06-27

Textbook Of Receptor Pharmacology Third Edition written by John C. Foreman and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2011-06-27 with Medical categories.


For the past four decades, University College London has offered a renowned course on receptor pharmacology. Originating from this course, the perennially bestselling Textbook of Receptor Pharmacology has presented in-depth coverage of this rapidly expanding area of research. This third edition continues to combine current understanding of classical quantitative pharmacology and drug-receptor interactions with the basics of receptor structure and signal transduction mechanisms, providing an integrated analysis of the mechanisms of drug action at membrane receptors. The hallmark of this popular text is the uniting of four major approaches to the study of receptors: Molecular investigation of receptor structure Quantitative functional studies of agonists and antagonists Ligand binding Signal transduction at the cell membrane Maintaining the second edition’s focus on cell membrane receptors and the immediate signal transduction events at the membrane, this edition includes updated chapters on receptor structure and signal transduction by G-proteins and tyrosine kinases as well as enhancements to the quantitative treatment of drug-receptor interactions. Several chapters contain problems and worked-out solutions, giving students the ability to test their comprehension of the material. Hundreds of diagrams and figures further enhance the text. A time-saving resource and comprehensive learning tool, Textbook of Receptor Pharmacology, Third Edition carries on the tradition of providing in-depth, up-to-date coverage of this critical area that is both fundamental to the science of pharmacology and on the cutting edge of new drug development.



G Protein Coupled Receptors


G Protein Coupled Receptors
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Author : Georges Vauquelin
language : en
Publisher: John Wiley & Sons
Release Date : 2008-03-11

G Protein Coupled Receptors written by Georges Vauquelin and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2008-03-11 with Medical categories.


G protein-coupled receptors (GPCRs) are membrane proteins that transduce a vast array of extracellular signals into intracellular reactions ranging from cell-cell communication processes to physiological responses. They play an important role in a variety of diseases from cancer and diabetes, to neurodegenerative, inflammatory and respiratory disorders. GPCRs are therefore of utmost interest in drug development: over half of all prescription drugs currently on the market act by targeting these receptors directly or indirectly. G Protein-coupled Receptors: Molecular Pharmacology provides a clear summary of the current knowledge in this fast-evolving field. The book sets out with an introduction to signalling molecules and their receptors, and an overview of the technical approaches used to investigate these interactions. Structural, functional and especially pharmacological aspects of GPCRs are then discussed in more detail and much attention is devoted to the analysis and interpretation of experimental data. The now widespread use of recombinant cell lies, receptor mutants and related artifices in drug research is critically evaluated. Special attention is also devoted to topical but often poorly understood concepts, such as insurmountable antagonism, inverse agonism and allosteric interactions. By combining general information with the major state-of-the-art concepts in GPCR-research, this outstanding book equips the reader with the necessary background for understanding and critically evaluating the current literature. Written by two experts from academia and industry, G Protein-coupled Receptors: Molecular Pharmacology offers a unique view of academic and applied approaches aiming to reveal new ideas in pharmaceutical research. The book is of interest to anyone involved in drug development and preclinical research and those who need to function within multi-disciplinary teams in the pharmaceutical industry: from investigators to product managers or clinicians who seek to have a broad mechanistic understanding of drug-receptor interactions. It is also an invaluable resource for final year undergraduate and postgraduate students in pharmacology and cell and molecular biology.



Principles In General Pharmacology


Principles In General Pharmacology
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Author : Ronald J. Tallarida
language : en
Publisher: Springer Science & Business Media
Release Date : 2012-12-06

Principles In General Pharmacology written by Ronald J. Tallarida and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012-12-06 with Medical categories.




Textbook Of Receptor Pharmacology


Textbook Of Receptor Pharmacology
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Author : John C. Foreman
language : en
Publisher: CRC Press
Release Date : 2010-09-10

Textbook Of Receptor Pharmacology written by John C. Foreman and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2010-09-10 with Medical categories.


For the past four decades, University College London has offered a renowned course on receptor pharmacology. Originating from this course, the perennially bestselling Textbook of Receptor Pharmacology has presented in-depth coverage of this rapidly expanding area of research. This third edition continues to combine current understanding of classica



The Dose Response Relation In Pharmacology


The Dose Response Relation In Pharmacology
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Author : Ronald Tallarida
language : en
Publisher: Springer
Release Date : 2012-03-29

The Dose Response Relation In Pharmacology written by Ronald Tallarida and has been published by Springer this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012-03-29 with Medical categories.


This book is designed to meet the modern need for a better understanding of drug-receptor interaction as applied to the gathering and interpretation of dose-response data. It is an introduction suitable for any student who has had a first course in pharmacology. This book is an extension of the pharmacology course into one area of what is now known as molecular pharmacology. The material included is an outgrowth of courses that we have given in recent years to health-science students in several professional schools and universities. The area of drug-receptor theory, although just a part of molecular phar macology, is already very broad. One major line of investigation is concerned with the chemical and structural nature of specific receptors and with efforts to isolate specific receptors. Another line of investigation is concerned with the kinetic theories of drug-receptor interaction, the effort there being to provide a general theory that is applicable to wide classes of drugs. We have chosen to deal with the latter. There are several reasons for our choice of topics. First, the information is very practical; that is, it permits one to use properly and consistently terms such as "efficacy," "partial agonist," "pure antagonist," "potency," "pA2'" etc., when describing drug action. Second, many students fail to appreciate the differences in and the limitations of the various theories, beginning with the classical theory of A. J. Clark, on up to the very recent allosteric theories.



Textbook Of Receptor Pharmacology Third Edition


Textbook Of Receptor Pharmacology Third Edition
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Author : John C. Foreman
language : en
Publisher: CRC Press
Release Date : 2010-09-10

Textbook Of Receptor Pharmacology Third Edition written by John C. Foreman and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2010-09-10 with Medical categories.


For the past four decades, University College London has offered a renowned course on receptor pharmacology. Originating from this course, the perennially bestselling Textbook of Receptor Pharmacology has presented in-depth coverage of this rapidly expanding area of research. This third edition continues to combine current understanding of classical quantitative pharmacology and drug-receptor interactions with the basics of receptor structure and signal transduction mechanisms, providing an integrated analysis of the mechanisms of drug action at membrane receptors. The hallmark of this popular text is the uniting of four major approaches to the study of receptors: Molecular investigation of receptor structure Quantitative functional studies of agonists and antagonists Ligand binding Signal transduction at the cell membrane Maintaining the second edition’s focus on cell membrane receptors and the immediate signal transduction events at the membrane, this edition includes updated chapters on receptor structure and signal transduction by G-proteins and tyrosine kinases as well as enhancements to the quantitative treatment of drug-receptor interactions. Several chapters contain problems and worked-out solutions, giving students the ability to test their comprehension of the material. Hundreds of diagrams and figures further enhance the text. A time-saving resource and comprehensive learning tool, Textbook of Receptor Pharmacology, Third Edition carries on the tradition of providing in-depth, up-to-date coverage of this critical area that is both fundamental to the science of pharmacology and on the cutting edge of new drug development.