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The Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems

  • Book
  • © 2000

Overview

Editors:
  1. Terry Kenakin

    1. Department of Receptor Biochemistry, Glaxo Wellcome Research and Development, USA

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    You can also search for this editor in PubMed   Google Scholar

  2. James A. Angus

    1. Department of Pharmacology, The University of Melbourne, Parkville, Australia

    View editor publications

    You can also search for this editor in PubMed   Google Scholar

Part of the book series: Handbook of Experimental Pharmacology (HEP, volume 148)

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Table of contents (16 chapters)

  1. Front Matter

    Pages I-XX
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  2. Introduction: Bioassays — Past Uses and Future Potential

    1. Introduction: Bioassays — Past Uses and Future Potential

      • J. W. Black
      Pages 1-11

  4. New Theoretical Concepts and Molecular Mechanisms of Receptor Function

    1. Front Matter

      Pages 117-117
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    2. Kinetic Modeling Approaches to Understanding Ligand Efficacy

      • J. J. Linderman
      Pages 119-146

    3. The Evolution of Drug-Receptor Models: The Cubic Ternary Complex Model for G Protein-Coupled Receptors

      • T. Kenakin, P. Morgan, M. Lutz, J. Weiss
      Pages 147-165

    4. Inverse Agonism

      • R. Bond, G. Milligan, M. Bouvier
      Pages 167-182

    5. Efficacy: Molecular Mechanisms and Operational Methods of Measurement. A New Algorithm for the Prediction of Side Effects

      • T. Kenakin
      Pages 183-216

    6. A Look at Receptor Efficacy. From the Signalling Network of the Cell to the Intramolecular Motion of the Receptor

      • H. O. Onaran, A. Scheer, S. Cotecchia, T. Costa
      Pages 217-259

    7. Mechanisms of Non-Competitive Antagonism and Co-Agonism

      • D. G. Trist, M. Corsi
      Pages 261-281

    8. Mechanisms of Receptor Activation and the Relationship to Receptor Structure

      • D. M. Perez, S. S. Karnik
      Pages 283-309
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Keywords

About this book

This, the 148th volume of the Handbook of Experimental Pharmacology series, focuses on the very core of pharmacology, namely receptor theory. It is fitting that the originator of receptor pharmacology, A. J. CLARK, authored the fourth volume of this series 63 years ago. In that volume CLARK further developed his version of receptor theory first described four years earlier in his classic book The Mode of Action of Drugs. An examination of the topics covered in volume 4 reveals a striking similarity to the topics covered in this present volume; pharmacologists today are still as interested in unlocking the secrets of dose-response relationships to reveal the biological and che­ mical basis of drug action as they were over half a century ago. Sections in that 1937 volume such as "Curves relating exposure to drugs with biological effects" and "Implications of monomolecular theory" show Clark's keen insight into the essential questions that required answers to move pharma­ cology forward. With the advent of molecular biological cloning of human receptors has come a transformation of receptor pharmacology. Thus the expression of human receptors into surrogate host cells helped unlock secrets of receptor mechanisms and stimulus-transduction pathways. To a large extent, this elim­ inates the leap of faith required to apply receptor activity of drugs tested on animal receptor systems to the human therapeutic arena. However, a new leap of faith concerning the veracity of the effects found in recombinant systems with respect to natural ones is now required.

Editors and Affiliations

  • Department of Receptor Biochemistry, Glaxo Wellcome Research and Development, USA

    Terry Kenakin

  • Department of Pharmacology, The University of Melbourne, Parkville, Australia

    James A. Angus

Bibliographic Information

  • Book Title: The Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems

  • Editors: Terry Kenakin, James A. Angus

  • Series Title: Handbook of Experimental Pharmacology

  • DOI: https://doi.org/10.1007/978-3-642-57081-0

  • Publisher: Springer Berlin, Heidelberg

  • eBook Packages: Springer Book Archive

  • Copyright Information: Springer-Verlag Berlin Heidelberg 2000

  • Hardcover ISBN: 978-3-540-66124-5Published: 15 August 2000

  • Softcover ISBN: 978-3-642-63028-6Published: 24 October 2012

  • eBook ISBN: 978-3-642-57081-0Published: 06 December 2012

  • Series ISSN: 0171-2004

  • Series E-ISSN: 1865-0325

  • Edition Number: 1

  • Number of Pages: XX, 448

  • Number of Illustrations: 131 b/w illustrations, 1 illustrations in colour

  • Topics: Pharmacology/Toxicology, Human Physiology, Biochemistry, general, Molecular Medicine

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