title: Characterization of the picrotoxin site of GABAA receptors.
abstract: This unit describes an in vitro assay for characterization of the picrotoxin site of GABAA 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.
authors: The University of Texas Health Science Center, San Antonio, Texas.
authors: Ashok K
authors: AK
authors: Mehta
authors: The University of Texas Health Science Center, San Antonio, Texas.
authors: Maharaj K
authors: MK
authors: Ticku
mesh_terms: D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000378:metabolism*; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000494:pharmacology; D002462:Cell Membrane / Q000378:metabolism; D018756:GABA Antagonists / Q000378:metabolism* / Q000493:pharmacokinetics; D010852:Picrotoxin / Q000378:metabolism* / Q000493:pharmacokinetics; D011869:Radioligand Assay / Q000379:methods; D051381:Rats; D011963:Receptors, GABA-A / Q000378:metabolism*
chemical_list: D019086:Bridged Bicyclo Compounds, Heterocyclic; D018756:GABA Antagonists; D010852:Picrotoxin; D011963:Receptors, GABA-A; C091518:1-(4-ethynylphenyl)-4-propyl-2,6,7-trioxabicyclo(2.2.2)octane; C046308:tert-butylbicyclo-2-benzoate
keywords: GABAA receptor; allosteric regulation; convulsants; picrotoxin binding site