Unit

UNIT 1.16 Benzodiazepine Binding to GABAA Receptors

  1. Dietmar Benke,
  2. Hanns Möhler

Published Online: 1 DEC 2006

DOI: 10.1002/0471141755.ph0116s35

Current Protocols in Pharmacology

Current Protocols in Pharmacology

How to Cite

Benke, D. and Möhler, H. 2006. Benzodiazepine Binding to GABAA Receptors. Current Protocols in Pharmacology. 35:1.16:1.16.1–1.16.14.

Author Information

  1. University of Zurich, Zurich, Switzerland

Publication History

  1. Published Online: 1 DEC 2006
  2. Published Print: NOV 2006

Abstract

This unit describes ligand binding assays for the characterization of the benzodiazepine (BZ) site of GABAA receptors in the central nervous system. The Basic Protocol provides a procedure for analyzing benzodiazepine binding to GABAA receptors from brain. The experimental design of the method is suitable for all commercially available radioligands that interact with the BZ site of central GABAA receptors. By using the appropriate radioligand in combination with particular displacer compounds, individual (or groups of) GABAA receptor subtypes can be identified. Preparation of membrane suspensions for this procedure is described in a Support Protocol, and five Alternate Protocols are provided for the identification of diazepam-sensitive GABAA receptors, the α1-subtype of diazepam-sensitive receptors, the α5 subtype of diazepam-sensitive receptors, both diazepam-sensitive and diazepam-insensitive receptors, and diazepam-insensitive receptors exclusively. Each protocol contains a brief description of the requirements for radioligand binding to these five types of BZ sites.

Keywords:

  • benzodiazepine;
  • BZ;
  • GABAA;
  • diazepam;
  • radioligand binding;
  • receptor subtype;
  • LGIC