Gaba receptor assays

GABAA Receptor Screening Services

Gaba receptor assays

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

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.

Gaba receptor screening assays

High throughput screening: Robust 384-well screening assays available using FLIPR or automated electrophysiology platforms.


Fluorescence Assays

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.

Gaba receptor assays
Gaba receptor assays

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).


Electrophysiology Assays

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.  

Gaba receptor assays
Gaba receptor assays

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.


Reproducibility

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.

Gaba receptor assays
Gaba receptor assays

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.

Gaba receptor assays
Gaba receptor assays

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
α1β1γ2 α1β2γ2 α1β3γ2 α4β3δ
α2β1γ2 α2β2γ2 α2β3γ2  
α3β1γ2 α3β2γ2 α3β3γ2  
α4β1γ2   α4β2γ2* α4β3γ2  
α5β1γ2 α5β2γ2 α5β3γ2  
α6β1γ2 α6β2γ2 α6β3γ2  
  *Coming soon    

To discuss your next ion channel project or to receive a quote, contact us or call +44 141 587 6100.


Ion channel cell lines
Contact SB