GABAA Receptor Screening Services
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) that have been shown to be vital for normal functioning of the brain. These inhibitory ligand-gated channels have been shown to be important in sedation, muscle relaxation and anaesthesia as well as being important drug targets for the treatment of neuronal disorders such as
epilepsy and anxiety.
SB Drug Discovery offers a comprehensive panel of GABAA assays for HTS, lead optimization studies and selectivity profiling. Our assays have been validated by experienced in-house electrophysiologists using rigorously optimized SOPs to ensure data of the highest quality and consistency.
High throughput screening using fluorescence and 384-well automated electrophysiology platforms enables rapid screening of compound sets for novel GABAA receptor modulators. SB's experienced screening team utilize high quality recombinant GABAA receptor-expressing cell lines to design, optimize and run high throughput screens targeting the GABAA subtype of your choice.
High throughput screening: Robust 384-well screening assays available using FLIPR or automated electrophysiology platforms.
Fluorescence assays using 96 & 384-well FLIPR platforms enable rapid screening of compound sets for novel GABAA receptor modulators. Assays can be run as single concentration screens or in dose-response format to assess modulation of response against a primary target or as part of a subtype selectivity panel.
GABAA receptor assays: Robust fluorescence-based FLIPR assays enable high throughput screening and selectivity profiling. Examples above show representative FLIPR traces from a GABAA receptor assay showing effect of increasing concentrations of GABA (left) and dose-dependent inhibition of GABAA α1-α6 (β1γ2) receptors (right).
Robust electrophysiology assays in 384-well plate format using the SyncroPatch 384PE facilitate generation of high quality electrophysiology data. Assays have been designed to assess agonists, antagonists and modulators of GABAA receptors with the ability to generate large electrophysiology datasets in short timeframes.
Automated electrophysiology assays: Validated 384-well electrophysiology assays enable detection and profiling of GABAA receptor agonists, antagonists and modulators. Examples show effect of EC50 & max GABA (left) and effect of positive allosteric modulator on GABA (EC10)-activated receptors.
High quality GABAA receptor cell lines enable complex assay set-ups including multiple repeat activation / wash steps enabling assessment of compounds with use-dependent properties.
High quality assays: GABAA SyncroPatch assays showing reproducible currents following repeat activation with GABA and / or GABA in the presence of test compound.
GABAA Subtype Selectivity Panels
Assess compound selectivity across a broad panel of GABAA subtypes using robust 384-well fluorescence or automated electrophysiology platforms. Choose from α or β specific selectivity panels, profile the entire GABAA panel or select a custom panel from any of our 18 GABAA subtypes. Agonist, antagonist and modulator assays are available to compare subtype selectivity using either FLIPR fluorescence assays or 384-well automated electrophysiology.
GABAA receptor selectivity panels: Examples show concentration-dependent effect of GABA on α1 - α6 (β1γ2) (left) and α1 - α6 (β2γ2) (right) expressing cells in a single plate electrophysiology assay.
GABAA Receptor Assays
|β1 subtypes||β2 subtypes||β3 subtypes||δ subtypes|
To discuss your next ion channel project or to receive a quote, contact us or call +44 141 587 6100.