Chapter 9. Constitutive Activity of β-Adrenoceptors: Analysis in Membrane Systems

  1. Prof. Roland Seifert1 and
  2. Prof. Thomas Wieland2
  1. Prof. Roland Seifert

Published Online: 25 APR 2006

DOI: 10.1002/352760734X.ch9

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

Seifert, R. (2005) Constitutive Activity of β-Adrenoceptors: Analysis in Membrane Systems, 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.ch9

Editor Information

  1. 1

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

  2. 2

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

Author Information

  1. Department of Pharmacology and Toxicology, University of Regensburg, Universitätsstraße 31, D-93053 Regensburg, 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 Mannhold3,
  2. Prof. Dr. Hugo Kubinyi4 and
  3. Prof. Dr. Gerd Folkers5

Series Editor Information

  1. 3

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

  2. 4

    Donnersbergstrasse 9, 67256 Weisenheim am Sand, Germany

  3. 5

    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);
  • constitutive activity of β-adrenoceptors;
  • analysis in membrane systems;
  • analysis of βAR/Gs protein coupling in membranes;
  • probing models of GPCR activation;
  • β2ARwt;
  • β2ARCAM;
  • inverse agonists;
  • purine nucleotides;
  • constitutive activity of the β2AR

Summary

This chapter contains sections titled:

  • Introduction

  • Analysis of βAR/Gs Protein Coupling in Membranes

  • Development of the Concept that βARs are Constitutively Active

  • Probing Models of GPCR Activation with β2ARwt and β2ARCAM with Inverse Agonists

  • Probing Models of GPCR Activation with β2ARwt and β2ARCAM and with Partial and Full Agonists

  • Probing Models of GPCR Activation with β2ARwt and Purine Nucleotides

  • Constitutive Activity of the β2AR Coupled to Various Gαs Proteins

  • Probing Models of GPCR Activation with β2AR Coupled to Various Classes of G proteins

  • Comparison of the Constitutive Activities of the β1AR and the β2AR

  • Conclusions