GABA_A Receptor (GABA_AR) Screening Service

GABA_A receptor (GABA_AR) is a kind of ligand-gated ion channel using endogenous γ-aminobutyric acid (GABA) as a ligand. Regarding the important role of the GABA_A receptor, reliable GABA_AR screening services are provided by Creative Biolabs, specialists in the field of ion channel screening, to facilitate the work of scientists worldwide.

Introduction of GABA_AR

GABA_ARs belong to the ligand-gated ion channel receptor superfamily for selectively chloride ion transduction. A central pore is surrounded by five subunits that make up the pentameric transmembrane GABA_ARs. Each subunit is made up of four transmembrane domains with the extracellular N- and C-termini. Once ligand GABA binds to the receptor, GABA_ARs will change their protein conformation, and the pore will switch to the open state for chloride ion influx. Bicarbonate ions are acceptable to a lesser extent. Given the wide distribution of GABA_AR on the neural cell membrane of postsynaptic synapses, the efficient operation of almost every component of the central nervous system depends on the precise control of GABA_AR-related ion transmission. The dysfunction of GABA_AR is tightly related to many neurodevelopmental diseases like the Rett syndrome, Dravet syndrome, and fragile X syndrome.

Fig.1 The structure of GABA_AR. Distributed under CC BY-SA 4.0, from Wiki, without modification.

GABA_AR Screening Service

The majority of GABA's physiological effects in the central nervous system are attributed to GABA_ARs. GABA_ARs have been recognized as promising therapeutic targets, which is not unexpected. GABA_AR screening is an advantageous approach for your in vitro pharmacological study of GABA_AR-related diseases and allows you to find potential modulators toward certain GABA_ARs that you are interested in.

For GABA_AR screening, correct establishment and validation of cell lines for your interested GABA_AR is the key to success. If you have specific candidates to test, electrophysiological methods like patch clamps will be a good choice because they generate physiologically relevant data with precise resolution. If you have a large scope of candidates, such as ligand library at the beginning of screening, a non-electrophysiological strategy, for instance, fluorescence-based assay, suits you better, for it is time-saving, cost-effective, and high-throughput. The high-throughput non-electrophysiological strategy can quickly and trustworthily find promising lead compounds.

Virtual screening can also be considered a way to uncover promising ligands of GABA_ARs due to its speed, cost, and high throughput.

Fig.2 Various ligands can bind to GABA_AR via binding different subunits. Distributed under Public Domain, from Wiki.

In humans, GABA_AR owns numerous subunit types, and the subunit compositions influence receptors' properties like agonist affinity. Constructing correct cell models means a lot for your custom GABA_AR screening project.

• α subunits, GABA_AR subunit alpha-1/2/3/4/5/6
• β subunits, GABA_AR subunit beta-1/2/3
• γ subunits, GABA_AR subunit gamma-1/2/3
• δ subunit, GABA_AR subunit delta
• ε subunit, GABA_AR subunit epsilon
• π subunit, GABA_AR subunit pi
• θ subunit, GABA_AR subunit theta

Features of Our Service

• Considerable expertise in ion channel screening and building bespoke cell models
• Specialized assay creation and customized assay approach
• One-stop service with assured quality and cost savings
• Thorough data analysis and top-notch after-sale assistance

To expedite your crucial research development, Creative Biolabs, which has vast expertise in GABA_AR screening research, can offer both electrophysiological and non-electrophysiological GABA_AR screening strategies, including virtual screening, on your interested GABA_ARs. Do not hesitate to contact us for more details.

In addition to GABA_AR Screening, Creative Biolabs also provides you with the following ligand-gated channel screening services

• CNG Channel Screening
• NMDA Receptor Screening
• nAChR Screening
• AMPAR Screening
• P2X Receptor Screening
• TRP Channel Screening
• Calcium-activated Channel Screening
• Sodium-activated Channel Screening

For Research Use Only. Not For Clinical Use.