PrecisION® hGABAA α1/β3/γ2 Recombinant Stable Cell Line

Gamma-aminobutyric acid (GABA)-gated ion channels are the major inhibitory neurotransmitter in the CNS, binding to fast-acting ionotropic GABAA receptors to cause inward flux of Cl- resulting in membrane hyperpolarization and thus reducing membrane excitability (Nutt et al., 2006). Excessive stimulation of these receptors can lead to sedation and ataxia whereas attenuation leads to arousal, insomnia and anxiety. Since modulation of these receptors has such profound physiological effects they have become important drug targets for the treatment of many conditions e.g. anxiety, epilepsy, sleep disorders and for anesthesia (Rudolph and Mohler, 2006). GABAA receptors are pentameric structures typically consisting of α, β and γ2 subunits in a stoichiometry of 2:2:1. The specific subunit composition is especially important since various combinations mediate different effects (Rudolph and Mohler, 2006). For example, α1-containing receptors, accounting for 60% of all GABAA receptors, mediate the sedative/hypnotic effects of benzodiazepines (BZPs) whereas the anxiolytic effects of these drugs are mediated by receptors containing α2 and α3 subunits (Korpi and Sinkkonen, 2006). Hence, developing selective allosteric modulators for these latter subunits should ultimately lead to anxiolytic drugs devoid of unwanted sedative effects.

Catalog No. Size Price Quantity
CYL3053 2 Vials Inquire

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Application
Electrophysiology assay (Conventional and automated patch clamp platforms)
Family
Chloride, Ligand-Gated
Target
GABAA α1/β3/γ2
Accession Number
NM_000806; NM_000814; NM_000816
Species
Human
Host Cell Type
HEK 293
Content
2 Vials of mycoplasma-free cells, 1 mL per vial aliquots containing 2M to 4M cells/mL in DMSO
Storage
Vials are to be stored in vapor phase of liquid N2