GABAA (alpha1/beta2/gamma2) Human Ion Channel Cell Based Antagonist APC LeadHunter Assay - US

Background Information:

The GABAA​ α1/β2/γ2 receptor is a heteropentameric, GABA‑gated chloride channel that contributes to fast synaptic inhibition in the brain and is a major target class for drugs used in epilepsy, anxiety, depression, insomnia, and anesthesia. These receptors are widely expressed across the CNS, including prominent expression in hippocampal and cerebellar neuronal populations (and broadly across the neuraxis at inhibitory synapses). Impaired GABAA signaling and altered receptor trafficking/expression are implicated in epilepsies (including genetic generalized epilepsies and developmental epileptic encephalopathies) and in psychiatric disorders where inhibitory balance is disrupted. At the gene/subunit level, GABRB3 (β2) and GABRG2 (γ2) are linked to neurodevelopmental epilepsy phenotypes, with β2 also tied to anxiety disorders, insomnia, psychiatric disorders, and altered cortical network function, while γ2 variants are classically associated with epilepsy syndromes such as GEFS+. The channel is sensitive to benzodiazepine-like compounds due to binding at the α1/γ2 interface . This assay identifies compounds that directly have antagonist effects on hGABAAα1/β2/γ2 channel expression in an acute timeframe.

Family:

Ion Channel

Sub Family:

GABAA

Class:

Ligand-Gated

Organism:

Human

Cell Type:

CHO-K1