Neurobiology
Positive and Negative Allosteric Modulation of an α1β3γ2 γ-Aminobutyric Acid Type A (GABAA) Receptor by Binding to a Site in the Transmembrane Domain at the γ+-β− Interface
Background: For some chiral barbiturates, one isomer potentiates and the other inhibits GABA responses by binding to unknown sites.Results: A photoreactive convulsant barbiturate identifies a transmembrane intersubunit-binding site between the γ and β subunits.Conclusion: Positive and negative allosteric modulators can bind to a common intersubunit site.Significance: This study defines a novel mode of regulation of GABAAR responses.
