Pharmacologic Analysis Of Drug Receptor Interaction
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Pharmacologic Analysis of Drug-receptor Interaction by Terrence P. Kenakin Pdf
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.
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. Contents:Ligand-Gated Ion Channels:Ligand-Gated Ion ChannelsAffinity and Efficacy of Orthosteric Ligands at Ligand-Gated Ion ChannelsCompetitive Interactions Between Orthostheric Ligands at Ligand-Gated Ion ChannelsAnalysis of Allosteric Interactions at Ligand-Gated Ion ChannelsG Protein-Coupled Receptors:G Protein-Coupled Receptors and G Protein and Arrestin SignalingAffinity and Efficacy of the Agonist-Receptor-G-Protein InteractionEstimating Affinity and Efficacy by Reverse-Engineering the Response-Clamp AnalysisAnalysis of Agonism and Inverse Agonism in Signaling Pathways that Exhibit Constitutive ActivityAnalysis of Ligand Bias in Receptor Signaling through Different G Protein PathwaysCompetitive Interactions Between Orthosteric Ligands in Functional Assays on G Protein-Coupled ReceptorsAnalysis of Allosterism in Functional Assays on G Protein-coupled ReceptorsRadioligand Binding:Analysis of Drug-receptor Interactions Using Radioligand Binding Assays on G Protein-coupled Receptors Readership: Postgraduates and researchers in pharmacology and physiology, professionals in the pharmaceutical industry, neuroscience researchers. Key Features:The concepts of receptor theory and hierarchical levels of pharmacological analysis are integrated and emphasised throughout the bookStep-by-step instructions are given for the different types of pharmacological analysesKeywords:Affinity;Efficacy;Drug-Receptor Interactions;Agonism;Antagonism;Allosterism;Binding;Ligand Directed Signaling;Pathway Selectivity;Inverse Agonism;G Protein-Coupled Receptors;Ligand-Gated Ion Channels;Cell Signaling
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.
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.
Drug-Acceptor Interactions: Modeling theoretical tools to test and evaluate experimental equilibrium effects suggests novel theoretical tools to test and evaluate drug interactions seen with combinatorial drug therapy. The book provides an in-depth, yet controversial, exploration of existing tools for analysis of dose-response studies at equilibrium or steady state. The book is recommended reading for post-graduate students and researchers engaged in the study of systems biology, networks, and the pharmacodynamics of natural or industrial drugs, as well as for medical clinicians interested in drug application and combinatorial drug therapy. Even people without mathematical skills will be able to follow the pros and cons of reaction schemes and their related distribution equations. Chapter 9 is a hands-on guide for software to plot, fit and analyze one’s own data.
Ronald J. Tallarida,Robert B. Raffa,Paul McGonigle
Author : Ronald J. Tallarida,Robert B. Raffa,Paul McGonigle Publisher : Springer Science & Business Media Page : 254 pages File Size : 54,6 Mb Release : 2012-12-06 Category : Medical ISBN : 9781461237785
Textbook of Receptor Pharmacology, Third Edition by John C. Foreman,Torben Johansen,Alasdair J. Gibb Pdf
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.
The Dose—Response Relation in Pharmacology by Ronald Tallarida,Leonard S. Jacob Pdf
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 by John C. Foreman,Torben Johansen,Alasdair J. Gibb Pdf
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
Author : Georges Vauquelin,Bengt von Mentzer Publisher : John Wiley & Sons Page : 264 pages File Size : 50,9 Mb Release : 2008-03-11 Category : Medical ISBN : 047051664X
G Protein-coupled Receptors by Georges Vauquelin,Bengt von Mentzer Pdf
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.
This guide has been designed especially for scientists trained in molecular biology and related fields who now need to know more about the basic theories, principles and practical applications of pharmacology.
Anesthetic Pharmacology by Alex S. Evers,Mervyn Maze,Evan D. Kharasch Pdf
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.
The Second Edition will continue this tradition of better preparing researchers in the basics of pharmacology. In addition, new human interest material including historical facts in pharmacology will be added. A new section on therapeutics will help readers identify with diseases and drug treatments. Over 30 new figures and tables More human interest information to provide readers with historical facts on pharmacology research New section on therapeutics to help identify diseaes and drug treatments New section on new biological concepts relevant to pharmacological research (i.e., systems biology) New study sections organized with ASPET and other international pharmacology organizations New coverage of pharmacokinetics and drug disposition
Textbook of Receptor Pharmacology, Third Edition by John C. Foreman,Torben Johansen,Alasdair J. Gibb Pdf
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.
