title: Characterization of the picrotoxin site of GABAA receptors.
abstract: This protocol describes an in vitro assay for characterization of the picrotoxin site of GABA(A) receptors in rat brain membranes using various radioligands. Methods and representative data for Scatchard analysis (Kd, Bmax determination), association kinetics, dissociation kinetics and competition assays (IC50, Ki determination) are included in the protocol.
authors.affiliation: The University of Texas Health Science Center, San Antonio, Texas, USA.
authors.forename: A K
authors.initials: AK
authors.lastname: Mehta
authors.forename: M K
authors.initials: MK
authors.lastname: Ticku
mesh_terms: D000818:Animals; D001665:Binding Sites; D001667:Binding, Competitive; D001923:Brain Chemistry; D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D007700:Kinetics; D008566:Membranes / Q000737:chemistry / Q000378:metabolism; D009570:Nitriles; D010852:Picrotoxin / Q000032:analysis* / Q000378:metabolism; D011869:Radioligand Assay / Q000379:methods*; D051381:Rats; D011963:Receptors, GABA-A / Q000032:analysis* / Q000378:metabolism; D013048:Specimen Handling; D013223:Statistics as Topic / Q000379:methods; D013462:Sulfur Radioisotopes; D005680:gamma-Aminobutyric Acid / Q000032:analysis* / Q000378:metabolism; D005466:Fluorocarbons
chemical_list: D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D009570:Nitriles; D010852:Picrotoxin; D011963:Receptors, GABA-A; D013462:Sulfur Radioisotopes; D005680:gamma-Aminobutyric Acid; C091518:1-(4-ethynylphenyl)-4-propyl-2,6,7-trioxabicyclo(2.2.2)octane; C037476:tert-butylbicyclophosphorothionate; C098123:3,3-bis(trifluoromethyl)bicyclo(2.2.1)heptane-2,2-dicarbonitrile; D005466:Fluorocarbons; C046308:tert-butylbicyclo-2-benzoate