© 2009

Functional Selectivity of G Protein-Coupled Receptor Ligands

New Opportunities for Drug Discovery

  • Kim A. Neve

Part of the The Receptors book series (REC)

Table of contents

  1. Front Matter
    Pages i-x
  2. Theoretical and Mechanistic Aspects of Functional Selectivity

  3. Subfamilies of Therapeutically Relevant Receptors

    1. Front Matter
      Pages 1-1
    2. Richard R. Neubig
      Pages 107-124
    3. Kelly A. Berg, William P. Clarke
      Pages 155-176
    4. Richard B. Mailman, Yan-Min Wang, Andrew Kant, Justin Brown
      Pages 177-209
    5. Graciela Piñeyro
      Pages 243-265
    6. Anushree Bhatnagar, Sadashiva Karnik
      Pages 267-281
  4. Back Matter
    Pages 283-290

About this book


Functional selectivity refers to the ability of different ligands acting at one receptor subtype to activate multiple signaling pathways in unique combinations; that is, one drug can be an agonist at pathway A and an antagonist or partial agonist at pathway B, and another drug can have the reverse profile. Functional selectivity has profound implications for drug development, for chemical biology, and for the design of experiments to characterize receptor function. In Functional Selectivity of G Protein-Coupled Receptors expert neuroscientists and pharmacologists review the work that demonstrated the existence of functional selectivity, placed it within a theoretical framework, and provided a mechanistic basis for the phenomenon. This exciting, comprehensive, and future-oriented volume includes chapters that focus on theoretical and mechanistic aspects of functional selectivity and that cut across subfamilies of GPCRs. Additional chapters focus on subfamilies of therapeutically relevant receptors where there is considerable evidence of ligand functional selectivity. Accessible and authoritative, Functional Selectivity of G Protein-Coupled Receptors is a valuable educational tool and reference source for students and scientists interested in drug development, chemical biology, and GPCR function.


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Editors and affiliations

  • Kim A. Neve
    • 1
  1. 1.Portland VA Medical Center (R & D-30)PortlandU.S.A.

Bibliographic information

Industry Sectors
Health & Hospitals


From the reviews:

“This book presents the current status of knowledge about ligand-specific intracellular signaling. … This book will be of greatest interest and utility to scientists actively involved in research into G protein-coupled receptors or drug discovery. … This is a … thorough, and detailed assessment of the current state of knowledge and recent developments in the field of G protein-coupled receptor function, signaling, and pharmacology.” (Beth Levant, Doody’s Review Service, December, 2009)

“Gives a comprehensive overview on all aspects of the functional selectivity concept of GPCR ligands … . It will help to generate more awareness for a key topic within the research community. … the volume at hand is of great educational benefit. … In general, the volume under review can be considered an excellent book … . can be an excellent companion for researchers just jumping into the field of GPCR agonist research, as well as for the expert scientist in the field.” (Christoph Boss, ChemMedChem, Vol. 5, 2010)