title: Benzodiazepine binding to GABA(A) receptors.
abstract: This unit describes ligand binding assays for the characterization of the benzodiazepine (BZ) site of GABA(A) receptors in the central nervous system. The Basic Protocol provides a procedure for analyzing benzodiazepine binding to GABA(A) receptors from brain. The experimental design of the method is suitable for all commercially available radioligands that interact with the BZ site of central GABA(A) receptors. By using the appropriate radioligand in combination with particular displacer compounds, individual (or groups of) GABA(A) 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 GABA(A) 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.
authors.affiliation: University of Zurich, Zurich, Switzerland.
authors.forename: Dietmar
authors.initials: D
authors.lastname: Benke
authors.forename: Hanns
authors.initials: H
authors.lastname: Möhler
mesh_terms: D001569:Benzodiazepines / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism*; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism*; D058785:GABA-A Receptor Agonists / Q000494:pharmacology; D058787:GABA-A Receptor Antagonists / Q000494:pharmacology; D006801:Humans; D008566:Membranes / Q000378:metabolism; D011869:Radioligand Assay / Q000379:methods*; D011963:Receptors, GABA-A / Q000378:metabolism*; D013048:Specimen Handling / Q000379:methods
chemical_list: D058785:GABA-A Receptor Agonists; D058787:GABA-A Receptor Antagonists; D011963:Receptors, GABA-A; D001569:Benzodiazepines