Affinity and Efficacy

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Author :
Publisher : World Scientific
ISBN 13 : 9814632163
Total Pages : 752 pages
Book Rating : 4.8/5 (146 download)

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Book Synopsis Affinity and Efficacy by : Frederick J Ehlert

Download or read book Affinity and Efficacy written by Frederick J Ehlert and published by World Scientific. This book was released on 2014-11-13 with total page 752 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Receptor-Receptor Interactions: A New Intramembrane Integrative Mechanism

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Author :
Publisher : Springer
ISBN 13 : 1349089494
Total Pages : 577 pages
Book Rating : 4.3/5 (49 download)

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Book Synopsis Receptor-Receptor Interactions: A New Intramembrane Integrative Mechanism by : Kjell Fuxe

Download or read book Receptor-Receptor Interactions: A New Intramembrane Integrative Mechanism written by Kjell Fuxe and published by Springer. This book was released on 2015-12-30 with total page 577 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Toxicant-Receptor Interactions

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Author :
Publisher : CRC Press
ISBN 13 : 143980592X
Total Pages : 243 pages
Book Rating : 4.4/5 (398 download)

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Book Synopsis Toxicant-Receptor Interactions by : Michael Denison

Download or read book Toxicant-Receptor Interactions written by Michael Denison and published by CRC Press. This book was released on 1998-08-10 with total page 243 pages. Available in PDF, EPUB and Kindle. Book excerpt: Many of the toxic effects elicited by xenobiotics can be explained at the molecular level by their interaction with receptors or by disruption or interference with receptor-mediated signal transduction pathways. This volume describes molecular approaches and reviews of current research. It provides reviews of numerous research areas which are direc

Receptor-Receptor Interactions

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Author :
Publisher : Academic Press
ISBN 13 : 0124104703
Total Pages : 539 pages
Book Rating : 4.1/5 (241 download)

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Book Synopsis Receptor-Receptor Interactions by : P. Michael Conn

Download or read book Receptor-Receptor Interactions written by P. Michael Conn and published by Academic Press. This book was released on 2013-10-18 with total page 539 pages. Available in PDF, EPUB and Kindle. Book excerpt: This new volume of Methods in Cell Biology looks at receptor-receptor interactions, with sections on allosteric and effector interactions, crystallization and modeling, measuring receptor-receptor interactions and oligomerization in individual classes. With cutting-edge material, this comprehensive collection is intended to guide researchers of receptor-receptor interactions for years to come. Covers sections on allosteric and effector interactions, crystallization and modeling, measuring receptor-receptor interactions and oligomerization in individual classes Chapters are written by experts in the field Cutting-edge material

Receptor Binding Techniques

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Author :
Publisher : Humana
ISBN 13 : 9781588294203
Total Pages : 240 pages
Book Rating : 4.2/5 (942 download)

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Book Synopsis Receptor Binding Techniques by : Anthony P. Davenport

Download or read book Receptor Binding Techniques written by Anthony P. Davenport and published by Humana. This book was released on 2005-03-25 with total page 240 pages. Available in PDF, EPUB and Kindle. Book excerpt: A comprehensive collection of readily reproducible methods for studying receptors in silico, in vitro, and in vivo. These cutting-edge techniques cover mining from curated databases, identifying novel receptors by high throughput screening, molecular methods to identify mRNA encoding receptors, radioligand binding assays and their analysis, quantitative autoradiography, and imaging receptors by positron emission tomography (PET). Highlights include phenotypic characterization of receptors in knockout mice, imaging receptors using green fluorescent protein and fluorescent resonance energy transfer, and quantitative analysis of receptor mRNA by TaqMan PCR. These book equips the researcher with techniques for exploring the unprecedented number of new receptor systems now emerging and the so-called "orphan" receptors whose activating ligand has not been identified.

Neurotransmitter-receptor Interactions

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Author :
Publisher :
ISBN 13 :
Total Pages : 628 pages
Book Rating : 4.:/5 (45 download)

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Book Synopsis Neurotransmitter-receptor Interactions by : D. J. Triggle

Download or read book Neurotransmitter-receptor Interactions written by D. J. Triggle and published by . This book was released on 1971 with total page 628 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Frontiers in Pharmacology of Neurotransmitters

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Publisher : Springer Nature
ISBN 13 : 9811535566
Total Pages : 729 pages
Book Rating : 4.8/5 (115 download)

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Book Synopsis Frontiers in Pharmacology of Neurotransmitters by : Puneet Kumar

Download or read book Frontiers in Pharmacology of Neurotransmitters written by Puneet Kumar and published by Springer Nature. This book was released on 2020-10-29 with total page 729 pages. Available in PDF, EPUB and Kindle. Book excerpt: Numerous phenomenal advances have been made towards understanding the role of neurotransmitters in the pathophysiology of neurological disorders, and these have resulted in a large number of novel molecules with the potential to revolutionize the treatment and prevention of such disorders. This book provides a comprehensive and detailed explanation of brain neurotransmitters and their receptors and associated channels. It includes a basic introduction, and also discusses the functions and recent advances and their pharmacology, highlighting the role of various computer aided drug design (CADD) strategies for the development of therapeutic ligands to modulate these receptors/ion channels. Written in an easy-to-read style, it is intended for neuroscience and pharmaceutical students and researchers working in the area of brain neurotransmitters.

Receptor-Receptor Interactions in the Central Nervous System

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Author :
Publisher : Humana
ISBN 13 : 9781493993314
Total Pages : 346 pages
Book Rating : 4.9/5 (933 download)

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Book Synopsis Receptor-Receptor Interactions in the Central Nervous System by : KJELL FUXE

Download or read book Receptor-Receptor Interactions in the Central Nervous System written by KJELL FUXE and published by Humana. This book was released on 2019-08-16 with total page 346 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume covers methodologies, ranging from the molecular level to the network level, used to study receptor-receptor interactions in heteroreceptor complexes inside the central nervous system. The chapters in this book cover topics such as biochemical binding techniques; receptor autoradiography; superfused synaptosome techniques; RTK-GPCR interaction; fluorescence and bioluminiscence energy transfer methods, Co-IP cytometry-based FRET; and novel bioinformatic approaches to understand membrane heteroreceptor complexes and the global panorama of their receptor-receptor interactions. In Neuromethods series style, chapters include the kind of detail and key advice from the specialists needed to get successful results in your laboratory. Cutting-edge and thorough, Receptor-Receptor Interactions in the Central Nervous System is a valuable resource for any scientist or researcher interested in this field of study.

Neuromorphic Olfaction

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Author :
Publisher : CRC Press
ISBN 13 : 1439871728
Total Pages : 237 pages
Book Rating : 4.4/5 (398 download)

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Book Synopsis Neuromorphic Olfaction by : Krishna C. Persaud

Download or read book Neuromorphic Olfaction written by Krishna C. Persaud and published by CRC Press. This book was released on 2016-04-19 with total page 237 pages. Available in PDF, EPUB and Kindle. Book excerpt: Many advances have been made in the last decade in the understanding of the computational principles underlying olfactory system functioning. Neuromorphic Olfaction is a collaboration among European researchers who, through NEUROCHEM (Fp7-Grant Agreement Number 216916)-a challenging and innovative European-funded project-introduce novel computing p

Receptor-ligand Interactions

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Author :
Publisher : Oxford University Press, USA
ISBN 13 :
Total Pages : 486 pages
Book Rating : 4.3/5 (91 download)

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Book Synopsis Receptor-ligand Interactions by : E. C. Hulme

Download or read book Receptor-ligand Interactions written by E. C. Hulme and published by Oxford University Press, USA. This book was released on 1992 with total page 486 pages. Available in PDF, EPUB and Kindle. Book excerpt: This is the final volume in a set of 3 books detailing practical methods for the investigation of biochemical receptors. This book deals with the performance and interpretation of receptor-ligand binding studies which are important in many areas of pharmacological and neurochemical research.

Textbook of Receptor Pharmacology

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Author :
Publisher : CRC Press
ISBN 13 : 1420052551
Total Pages : 314 pages
Book Rating : 4.4/5 (2 download)

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Book Synopsis Textbook of Receptor Pharmacology by : John C. Foreman

Download or read book Textbook of Receptor Pharmacology written by John C. Foreman and published by CRC Press. This book was released on 2010-09-10 with total page 314 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Pharmacologic Analysis of Drug-receptor Interaction

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Author :
Publisher : Raven Press (ID)
ISBN 13 :
Total Pages : 504 pages
Book Rating : 4.3/5 (91 download)

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Book Synopsis Pharmacologic Analysis of Drug-receptor Interaction by : Terrence P. Kenakin

Download or read book Pharmacologic Analysis of Drug-receptor Interaction written by Terrence P. Kenakin and published by Raven Press (ID). This book was released on 1993 with total page 504 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Fundamental Concepts in Drug-receptor Interactions

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Author :
Publisher :
ISBN 13 :
Total Pages : 280 pages
Book Rating : 4.:/5 (43 download)

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Book Synopsis Fundamental Concepts in Drug-receptor Interactions by : James Frederic Danielli

Download or read book Fundamental Concepts in Drug-receptor Interactions written by James Frederic Danielli and published by . This book was released on 1970 with total page 280 pages. Available in PDF, EPUB and Kindle. Book excerpt:

G Protein-coupled Receptors

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Author :
Publisher : John Wiley & Sons
ISBN 13 : 9780470516645
Total Pages : 264 pages
Book Rating : 4.5/5 (166 download)

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Book Synopsis G Protein-coupled Receptors by : Georges Vauquelin

Download or read book G Protein-coupled Receptors written by Georges Vauquelin and published by John Wiley & Sons. This book was released on 2008-03-11 with total page 264 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Receptor Regulation

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Publisher : Springer Science & Business Media
ISBN 13 : 9400958226
Total Pages : 258 pages
Book Rating : 4.4/5 (9 download)

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Book Synopsis Receptor Regulation by : R. J. Lefkowitz

Download or read book Receptor Regulation written by R. J. Lefkowitz and published by Springer Science & Business Media. This book was released on 2013-03-09 with total page 258 pages. Available in PDF, EPUB and Kindle. Book excerpt: ROBERT J. LEFKOWITZ, M. D. Receptor Regulation (Receptors and Recognition, Series B, Volume 13) Edited by R. J. Lefkowitz Published in 1981 by Chapman and Hall, 11 New Fetter Lane, London EC4P 4EE © 1981 Chapman and Hall The study of hormone and drug receptors has become one of the most excit ing and rapidly moving areas of biomedical research. Elucidation of receptor mechanisms and receptor structure has become the common goal of many scientists from diverse backgrounds. The rapid advances achieved have been due, in large part, to the concentrated effort of workers from a variety of disciplines including classical pharmacology, biochemistry, endocrinology, cell biology, genetics' and molecular biology, among others. Hormone and drug receptors appear to be of three major types, which may be classified by their cellular locations. Found in the plasma membranes of cells are the receptors for a wide variety of polypeptide hormones, catecholamines and a variety of neurotransmitters. Included within this group are those receptors coupled to the enzyme adenylate cyclase. The second group of receptors are the soluble cytoplasmic receptors for the steroid hormones. A third type of hormone receptor is the receptor for the thyroid hormones which appears to be confined to the nucleus. Not only may these different types of receptor be distinguished in terms of their cellular locations but also by their mechanisms of action.

Hormone-receptor Interaction

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Publisher :
ISBN 13 :
Total Pages : 496 pages
Book Rating : 4.3/5 (91 download)

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Book Synopsis Hormone-receptor Interaction by : Gerald S. Levey

Download or read book Hormone-receptor Interaction written by Gerald S. Levey and published by . This book was released on 1976 with total page 496 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Drug-Receptor Thermodynamics

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Author :
Publisher : Wiley
ISBN 13 : 9780471720423
Total Pages : 0 pages
Book Rating : 4.7/5 (24 download)

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Book Synopsis Drug-Receptor Thermodynamics by : Robert B. Raffa

Download or read book Drug-Receptor Thermodynamics written by Robert B. Raffa and published by Wiley. This book was released on 2001-06-08 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug-Receptor Thermodynamics is the first book to provide in depth coverage of principles and applications of thermodynamic drug-receptor interactions. The book starts from familiar points, making thermodynamics accessible to anyone interested in how drugs work. The ideas presented cover general principles as well as laying the groundwork for new ways of examining drug action. * covers an area of increasing interest and relevance in the field of drug design and discovery * excellent explanation of why thermodynamics is at the heart of drug action * contributions from many of the worlds leading experts in the field Anyone interested in drug receptor interaction will find something of use in this book. It will be of particular relevance for pharmacologists, health science researchers and medicinal chemists.