GABAA receptors are vital for controlling neuronal excitability and can display significant
levels of constitutive activity that contributes to tonic inhibition. However, the mechanisms …

The diversity of GABAA receptor (GABAAR) subunits and the numerous configurations
during subunit assembly give rise to a variety of receptors with different functional properties …

GABAA receptors mediate synaptic and extrasynaptic inhibition. Native receptors consist of
α and β subunits, which are required for function, and another “modulatory” subunit, for …

GABA receptors (GABAARs) mediate inhibition in the adult brain. These channels are
heteropentamers and their ligand binding sites are localized at the β (+)/α (−) interfaces. As …

GABAA receptor function can be conceptually divided into interactions between ligand and
receptor (binding) and the opening and closing of the ligand-bound channel (gating). The …

Protein movements underlying ligand-gated ion channel activation are poorly understood.
The binding of agonist initiates a series of conformational movements that ultimately lead to …

GABA (γ-aminobutyric acid) B receptors are heterodimeric G protein–coupled receptors that
mediate slow synaptic inhibition in the central nervous system. Here we show that the …

Key points Physiologically relevant combinations of recombinant GABAA receptor (GABAR)
subunits were expressed in HEK293 cells. Using whole‐cell voltage clamp and rapid drug …

The expression of GABAA receptors and the efficacy of GABAergic neurotransmission are
subject to adaptive compensatory regulation as a result of changes in neuronal activity …

2006). The subunit composition (two α, two β and another) determines the pharmacological
and kinetic characteristics of the receptor. Certain combinations, such as α6βδ, α4βδ and …