Chapter 10. Constitutive Activity of β-Adrenoceptors: Analysis by Physiological Methods

  1. Prof. Roland Seifert4 and
  2. Prof. Thomas Wieland5
  1. Ursula Ravens1,
  2. Clive J. Lewis2 and
  3. Sian E. Harding3

Published Online: 25 APR 2006

DOI: 10.1002/352760734X.ch10

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

Ravens, U., Lewis, C. J. and Harding, S. E. (2006) Constitutive Activity of β-Adrenoceptors: Analysis by Physiological Methods, 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.ch10

Editor Information

  1. 4

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

  2. 5

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

Author Information

  1. 1

    Institut für Pharmakologie und Toxikologie, Technische Universität Dresden, Fetscherstr. 74, 01307 Dresden, Germany

  2. 2

    St Georges Hospital, Blackshaw Road, Tooting, London, SW17 OQT, United Kingdom

  3. 3

    National Heart and Lung Institute, Imperial College School of Medicine, Dovehouse Street, London SW3 6LY, United Kingdom

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 Mannhold6,
  2. Prof. Dr. Hugo Kubinyi7 and
  3. Prof. Dr. Gerd Folkers8

Series Editor Information

  1. 6

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

  2. 7

    Donnersbergstrasse 9, 67256 Weisenheim am Sand, Germany

  3. 8

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

ISBN Information

Print ISBN: 9783527308194

Online ISBN: 9783527607341

SEARCH

Keywords:

  • G protein coupled receptors (GPCR);
  • constitutive activity of β-adrenoceptors;
  • analysis by physiological methods;
  • inverse agonism;
  • β2-adrenoceptors;
  • β1-adrenoceptors;
  • homo- and heterodimerization

Summary

This chapter contains sections titled:

  • Introduction

  • Constitutive Activity and Inverse Agonism: Definition and Detection

  • β1-Adrenoceptors

    • Constitutive Activity of Overexpressed β1ARs

    • Is there any Evidence for a Physiological Effect of Constitutively Active Receptors in Normal Cardiomyocytes?

    • Substates of the β1AR: the Putative β4AR

  • β2-Adrenoceptors

    • Constitutive Activity of Overexpressed β2ARs

    • Inverse Agonism at the β2AR

    • βAR Antagonists: Inverse Agonists at β2AR-Gs or Full Agonists at β2AR-Gi?

    • Involvement of the β2AR in the “Putative β4AR” Effect

  • Homo- and Heterodimerization of β1- and β2ARs

  • Conclusions