Application note: GABAA Receptors
SB Drug Discovery shows the validation of fluorescence and automated electrophysiology assays designed to assess agonists, antagonists and allosteric modulators of these receptors, culminating in a high-throughput electrophysiology assay suited to assessing multiple GABAA receptor subtypes on a single assay plate.
GABAA receptors represent a large and complex family of ion channels that consist of at least 16 subunits (α1-6, β1-3, γ1-3, δ, ε, π, θ) and have been shown to be vital for the normal functioning of the brain. These ligand-gated chloride ion channels form pentameric structures and are activated by γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the CNS, resulting in an inhibitory effect on neurotransmission.
GABAA receptors have been shown to be important in sedation, muscle relaxation and anaesthesia as well as being key drug targets for the treatment of neuronal disorders such as epilepsy and anxiety.