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Affinity and Efficacy

Affinity and Efficacy
Author: Frederick J. Ehlert
Publisher: World Scientific Publishing Company Incorporated
Total Pages: 739
Release: 2014-09-15
Genre: Medical
ISBN: 9789814322560

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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.


Toxicant-Receptor Interactions

Toxicant-Receptor Interactions
Author: Michael Denison
Publisher: CRC Press
Total Pages: 243
Release: 1998-08-10
Genre: Medical
ISBN: 143980592X

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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

Receptor-Receptor Interactions
Author: P. Michael Conn
Publisher: Academic Press
Total Pages: 539
Release: 2013-10-18
Genre: Science
ISBN: 0124104703

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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

Receptor Binding Techniques
Author: Anthony P. Davenport
Publisher: Humana
Total Pages: 240
Release: 2005-03-25
Genre: Medical
ISBN: 9781588294203

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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.


Receptor-Receptor Interactions in the Central Nervous System

Receptor-Receptor Interactions in the Central Nervous System
Author: KJELL FUXE
Publisher: Humana
Total Pages: 346
Release: 2019-08-16
Genre: Medical
ISBN: 9781493993314

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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.


Frontiers in Pharmacology of Neurotransmitters

Frontiers in Pharmacology of Neurotransmitters
Author: Puneet Kumar
Publisher: Springer Nature
Total Pages: 729
Release: 2020-10-29
Genre: Medical
ISBN: 9811535566

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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.


Neuromorphic Olfaction

Neuromorphic Olfaction
Author: Krishna C. Persaud
Publisher: CRC Press
Total Pages: 237
Release: 2016-04-19
Genre: Medical
ISBN: 1439871728

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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

Receptor-ligand Interactions
Author: E. C. Hulme
Publisher: Oxford University Press, USA
Total Pages: 486
Release: 1992
Genre: Medical
ISBN:

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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.