Chapter 7. (Patho)physiological and Therapeutic Relevance of Constitutive Activity and Inverse Agonism at G Protein-Coupled Receptors

  1. Prof. Roland Seifert2 and
  2. Prof. Thomas Wieland3
  1. Lutz Hein

Published Online: 25 APR 2006

DOI: 10.1002/352760734X.ch7

G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity, Volume 24

G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity, Volume 24

How to Cite

Hein, L. (2005) (Patho)physiological and Therapeutic Relevance of Constitutive Activity and Inverse Agonism at G Protein-Coupled Receptors, in G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity, Volume 24 (eds R. Seifert and T. Wieland), Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, FRG. doi: 10.1002/352760734X.ch7

Editor Information

  1. 2

    Department of Pharmacology and Toxicology, University of Regensburg, Universitätsstraße 31, D-93053 Regensburg, Germany

  2. 3

    Institut für Pharmakologie und Toxikologie, Fakultät für Klinische Medizin Mannheim der Universität Heidelberg, Maybachstraße 14-16, 68169 Mannheim, Germany

Author Information

  1. Institut für Experimentelle und Klinische Pharmakologie und Toxikologie, Universität Freiburg, Albertstraße 25, 79104 Freiburg, Germany

Publication History

  1. Published Online: 25 APR 2006
  2. Published Print: 26 SEP 2005

Book Series:

  1. Methods and Principles in Medicinal Chemistry

Book Series Editors:

  1. Prof. Dr. Raimund Mannhold4,
  2. Prof. Dr. Hugo Kubinyi5 and
  3. Prof. Dr. Gerd Folkers6

Series Editor Information

  1. 4

    Biomedical Research Center, Molecular Drug Research Group, Heinrich-Heine-Universität, Universitätsstrasse 1, 40225 Düsseldorf, Germany

  2. 5

    Donnersbergstrasse 9, 67256 Weisenheim am Sand, Germany

  3. 6

    Collegium Helveticum, STW/ETH Zentrum, 8092 Zürich, Switzerland

ISBN Information

Print ISBN: 9783527308194

Online ISBN: 9783527607341

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Keywords:

  • G protein coupled receptors (GPCR);
  • physiological relevance;
  • constitutive activity of GPCRs;
  • pathophysiology of disease;
  • physiological relevance of inverse agonists;
  • inverse agonists as drugs

Summary

This chapter contains sections titled:

  • Introduction

  • Physiological Relevance of Constitutive Activity of GPCRs

  • Constitutive Activity of GPCRs and Pathophysiology of Disease

  • Physiological Relevance of Inverse Agonists

  • Inverse Agonists as Drugs

  • Conclusions