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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.
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
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.
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 thoroughly revised, updated Third Edition of this highly acclaimed text reflects the past four years' groundbreaking developments in receptor pharmacology, particularly the use of human recombinant receptor systems in drug design and development. Whereas prior editions focused on the correspondence of animal to human receptor systems, this new edition examines drug effects on human receptors obtained by recombinant technology, as well as on physiological natural receptor systems in animals. Two new chapters explain how to produce and use human recombinant receptor systems and discuss the interpretation of data from human recombinant receptor studies. Other chapters describe the use of receptor studies to measure and characterize the biological actions of drugs.
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.
This exciting volume elucidates how GPCRs organize signal transduction and control intracellular activities. Chapters written by the recognized expert in each respective topic offer state-of-the-art updates on the principles and technology, as well as stepwise protocols for methods currently applied to the analysis of protein-receptor interactions.
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.
This is the last in a set of three books covering the practical aspects of receptor biochemistry, receptor-effector coupling, and neurotransmitter/hormone receptor-ligand interactions. It focuses on the preparation, performance and interpretation of receptor-ligand binding studies, which are widely used in mainstream pharmacology, both in academic laboratories and the pharmaceutical industry. Binding studies are difficult to effectively perform, hence expert guidance and many practical tips are given throughout. The book contains a wealth of valuable protocols, and will be a useful bench manual for researchers in pharmacology, neuroscience, molecular biology and biochemistry.