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Author: Frederick J. Ehlert Publisher: World Scientific Publishing Company Incorporated ISBN: 9789814322560 Category : Medical Languages : en Pages : 739
Book Description
The interaction of a drug with a receptor encodes a vector 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 drugreceptor 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 shed 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, ligand-directed signaling, modulation of pathway selectivity, and the analysis of the loss of function in tissues from receptor knockout mice. The natural history and structure of ligand-gated ion channels, G proteins, and G protein-coupled receptors are also discussed.
Author: Frederick J Ehlert Publisher: World Scientific ISBN: 9814632163 Category : Medical Languages : en Pages : 750
Book Description
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.
Author: P. Michael Conn Publisher: Academic Press ISBN: 0124104703 Category : Science Languages : en Pages : 539
Book Description
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
Author: Anthony P. Davenport Publisher: Humana ISBN: 9781588294203 Category : Medical Languages : en Pages : 240
Book Description
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.
Author: Michael Denison Publisher: CRC Press ISBN: 9781439805923 Category : Medical Languages : en Pages : 260
Book Description
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
Author: Puneet Kumar Publisher: Springer Nature ISBN: 9811535566 Category : Medical Languages : en Pages : 729
Book Description
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.