Receptor - Based Drug Design  book cover
1st Edition

Receptor - Based Drug Design

ISBN 9780367400521
Published September 23, 2019 by CRC Press
400 Pages

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Book Description

Employing a wide range of examples from G-protein-coupled receptors and ligand-gated ion channels, this detailed, single-source reference illustrates the principles of pharmacological analysis and receptor classification that are the basis of rational drug design.
Explains the experimental and theoretical methods used to characterize interactions between ligands and receptors-providing the pharmacological information needed to solve treatment problems and facilitate the drug design process!
Demonstrating the achievements of the receptor-based approach in therapeutics and indicating future directions, Receptor-Based Drug Design

  • introduces novel computer-assisted strategies for the design of new agonists, antagonists, and inverse agonists for G-protein-coupled receptors
  • shows how to assess agonist concentration-effect curve data
  • discusses radioligand binding assays
  • presents new in vitro multiarray assays for G-protein-coupled receptors
  • explains the use of individual second messenger signaling responses in analyzing drug-receptor interactions
  • examines the role of electrophysiology in finding new drugs and drug targets
  • describes selectively acting b-adrenoceptor agonists and glucocorticoid steroids for asthma treatment
  • outlines the rationale for using angiotensin receptor antagonists
  • and more!
    Written by over 25 international authorities and containing nearly 1200 bibliographic citations, Receptor-Based Drug Design is a practical resource for pharmacologists, pharmacists, and pharmaceutical scientists; organic and medicinal chemists and biochemists; molecular biologists; biomedical researchers; and upper-level undergraduate and graduate students in these disciplines.
  • Table of Contents

    Introduction, James Black

    Principles and Measurement of Drug-Receptor Interactions

    The Characterization and Classification of Receptors, Patrick P. A. Humphrey
    Functional Methods for Quantifying Agonists and Antagonists, Iain G. Dougall
    Quantification of Receptor Interactions Using Binding Methods, Sebastian Lazareno
    Drug Analysis Based on Signaling Responses to G-Protein-Coupled Receptors, T. Kendall Harden, José L. Boyer, and Robert W. Dougherty
    The Use of Electrophysiology to Improve Understanding of Drug-Receptor Interactions, John G. Connolly and Charles Kennedy

    Receptor-Based Drugs in Medicine

    Selective Adrenergic and Glucocorticoid Treatments for Asthma, David Jack
    Serotonin 5-HT1B/D Receptor Agonists, Graeme R. Martin
    Histamine H2-Receptor Antagonists, Michael E. Parsons
    Angiotensin Antagonists, Mark J. Robertson

    Experimental and Emerging Drugs

    -Adrenoceptor Agonists and Antagonists, J. Paul Hieble and Robert R. Ruffolo, Jr.
    P2U-Purinoceptor Agonists: Emerging Therapy for Pulmonary Diseases, Eduardo R. Lazarowski, William C. Watt, T. Kendall Harden, and Richard C. Boucher
    Muscarinic Receptor Antagonists Pharmacological and Therapeutic Utility, Richard M. Eglen
    NMDA Receptor Antagonists, John A. Kemp and James N. C. Kew

    New Trends in Drug Design

    Computational Chemistry in Receptor-Based Drug Design, Ad P. IJzerman, Eleonora M. van der Wenden, and Wilma Kuipers
    Recombinant G-Protein-Coupled Receptors as Screening Tools for Drug Discovery, A. Donny Strosberg and Prabhavathi B. Fernandes
    Inverse Agonists and G-Protein-Coupled Receptors, Richard A. Bond and Michel Bouvier

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    Leff Paul