GABA-A α1β2γ2 human Ion Channel [3H] Ro-15-1788 Binding LeadHunter Assay - TW

Background Information:

The GABA-A α1β2γ2 receptor is a ligand-gated chloride channel of the Cys-loop superfamily, assembled as a pentamer of α1, β2, and γ2 subunits (2α:2β:1γ) with TM2 segments lining the central chloride-selective pore. The most abundant GABA-A subtype in the adult brain, it predominates at postsynaptic inhibitory synapses across the cortex, hippocampus, cerebellum, and thalamus. GABA binding at α1–β2 interfaces triggers chloride influx, suppressing neuronal excitability to regulate sleep, anxiety, and seizure threshold. The γ2 subunit confers synaptic clustering and benzodiazepine sensitivity. Loss-of-function mutations in GABRA1, GABRB2, or GABRG2 cause genetic generalized epilepsies including Dravet syndrome. Pharmacologically, benzodiazepines (e.g., diazepam) positively modulate the α1–γ2 interface enhancing chloride conductance, barbiturates such as phenobarbital extend channel open duration via the TM2 pore region, and anesthetics including propofol and etomidate potentiate activity at transmembrane β2–α1 sites. Competitive antagonist bicuculline and non-competitive blocker picrotoxin serve as essential research tools. The α1β2γ2 receptor thus represents a critical target for antiepileptic, anxiolytic, and anesthetic drug development and CNS safety pharmacology assessment.

Family:

Ion Channel

Sub Family:

Chloride

Class:

Ligand-Gated

Protein Name:

GBRA1

Uniprot Number:

P14867

Protein Aliases:

GABA(A) receptor subunit alpha-1, GABAAR subunit alpha-1 | GABA(A) receptor subunit beta-2, GABAAR subunit beta-2 | GABA(A) receptor subunit gamma-2, GABAAR subunit gamma-2

Gene Name:

GABRA1

Gene ID:

2554

Gene Aliases:

DEE19, ECA4, EIEE19, EJM, EJM5

Organism:

Human