Affinity And Efficacy: The Components Of Drug-receptor Interactions

Affinity And Efficacy: The Components Of Drug-receptor Interactions
Author: Frederick J Ehlert
Publisher: World Scientific
Total Pages: 750
Release: 2014-11-13
Genre: Medical
ISBN: 9814632163

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.

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

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.

Drug-Acceptor Interactions

Drug-Acceptor Interactions
Author: Niels Bindslev
Publisher: CRC Press
Total Pages: 847
Release: 2017-02-10
Genre: Medical
ISBN: 1351660578

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.

Guidelines for the Psychosocially Assisted Pharmacological Treatment of Opioid Dependence

Guidelines for the Psychosocially Assisted Pharmacological Treatment of Opioid Dependence
Author: World Health Organization. Department of Mental Health and Substance Abuse
Publisher: World Health Organization
Total Pages: 133
Release: 2009
Genre: Medical
ISBN: 9241547545

"These guidelines were produced by the World Health Organization (WHO), Department of Mental Health and Substance Abuse, in collaboration with the United Nations Office on Drugs and Crime (UNODC) a Guidelines Development Group of technical experts, and in consultation with the International Narcotics Control Board (INCB) secretariat and other WHO departments. WHO also wishes to acknowledge the financial contribution of UNODC and the Joint United Nations Programme on HIV/AIDS (UNAIDS) to this project. " - p. iv

Anesthetic Pharmacology

Anesthetic Pharmacology
Author: Alex S. Evers
Publisher: Cambridge University Press
Total Pages: 2902
Release: 2011-03-10
Genre: Medical
ISBN: 1139497022

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.

Encyclopedic Reference of Molecular Pharmacology

Encyclopedic Reference of Molecular Pharmacology
Author: Stefan Offermanns
Publisher:
Total Pages: 1152
Release: 2004
Genre: Medical
ISBN:

Presents current information on the molecular mechanisms of drug action. Provides 159 essays describing groups of drugs and drug targets. Several essays deal with general principles of pharmacology, such as drug tolerance, drug addiction, or drug metabolism.

Fundamentals of Anaesthesia

Fundamentals of Anaesthesia
Author: Colin Pinnock
Publisher: Cambridge University Press
Total Pages: 990
Release: 2002-12
Genre: Medical
ISBN: 9780521690799

The second edition of Fundamentals of Anaesthesia builds upon the success of the first edition, and encapsulates the modern practice of anaesthesia in a single volume. Written and edited by a team of expert contributors, it provides a comprehensive but easily readable account of all of the information required by the FRCA Primary examination candidate and has been expanded to include more detail on all topics and to include new topics now covered in the examination. As with the previous edition, presentation of information is clear and concise, with the use of lists, tables, summary boxes and line illustrations where necessary to highlight important information and aid the understanding of complex topics. Great care has been taken to ensure an unrivalled consistency of style and presentation throughout.

Thermodynamics and Kinetics of Drug Binding

Thermodynamics and Kinetics of Drug Binding
Author: György Keserü
Publisher: John Wiley & Sons
Total Pages: 360
Release: 2015-08-17
Genre: Medical
ISBN: 352733582X

This practical reference for medicinal and pharmaceutical chemists combines the theoretical background with modern methods as well as applications from recent lead finding and optimization projects. Divided into two parts on the thermodynamics and kinetics of drug-receptor interaction, the text provides the conceptual and methodological basis for characterizing binding mechanisms for drugs and other bioactive molecules. It covers all currently used methods, from experimental approaches, such as ITC or SPR, right up to the latest computational methods. Case studies of real-life lead or drug development projects are also included so readers can apply the methods learned to their own projects. Finally, the benefits of a thorough binding mode analysis for any drug development project are summarized in an outlook chapter written by the editors.