13. Constitutively Active Histamine Receptors

  1. Prof. Roland Seifert2 and
  2. Prof. Thomas Wieland3
  1. Remko A. Bakker and
  2. Rob Leurs

Published Online: 25 APR 2006

DOI: 10.1002/352760734X.ch13

G Protein‐Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity

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

How to Cite

Bakker, R. A. and Leurs, R. (2005) Constitutively Active Histamine Receptors, in G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity (eds R. Seifert and T. Wieland), Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, FRG. doi: 10.1002/352760734X.ch13

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. Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Faculty of Chemistry, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands

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);
  • constitutively active histamine receptors;
  • assay systems;
  • detection

Summary

This chapter contains sections titled:

  • Introduction

  • The Histamine Receptors

    • The H1R

    • The H2R

    • The H3R

    • The H4R

  • Assay Systems for Detection of Constitutive Activity of Histamine Receptors

    • Histamine Receptor Expression and the Detection of Constitutive Activity

    • Changes in Intracellular Ca2+

    • [35S]GTPγS Binding Assays (see also Chapter 8)

    • IP3 Formation (see also Chapter 8)

    • cAMP Assays (see also Chapter 8)

    • Measurements of Arachidonic Acid (AA) Release

    • Reporter Gene Assays (see also Chapter 8)

    • Activation of Kinases

    • Effects of the Cellular Environment on Histamine Receptor Activity

    • Construction and Expression of Constitutively Active Mutant Receptors

    • Contamination with Endogenous Histamine

  • Conclusions