At Creative Biolabs, we are committed to advancing drug discovery by providing high-quality, comprehensive assay services for a wide array of ion channels. We are committed to helping you unlock the potential of GABAA channel research with reliable, customized assay services.

GABAA Channels

The GABAA receptor channel is a critical component of the central nervous system, functioning primarily as an inhibitory neurotransmitter receptor. This ion channel is activated by GABA, the principal inhibitory neurotransmitter in the mammalian brain, leading to the opening of a chloride ion channel. Upon activation, the influx of chloride ions hyperpolarizes the neuron, making it less likely to fire an action potential, thereby exerting a calming effect on neuronal activity. The GABAA receptor is a target for various pharmacological agents, including benzodiazepines, barbiturates, and anesthetics, which modulate its activity to achieve therapeutic effects such as anxiolysis, sedation, and muscle relaxation. Its role in maintaining the balance between neuronal excitation and inhibition is crucial for normal brain function, and dysregulation of GABAA channels is implicated in several neurological and psychiatric disorders, including anxiety, epilepsy, and insomnia.

Fig.1 Structure of ionotropic GABAA receptors.¹

Comprehensive Screening Capabilities

Creative Biolabs utilizes cutting-edge technologies to deliver reliable and reproducible results in GABAA channel research. Our electrophysiology team has extensive experience with automated patch-clamp and manual patch-clamp studies, providing precise measurements of ion channel activity. These methods are particularly advantageous for studying the intricate dynamics of GABAA channels and their response to different pharmacological agents. We also incorporate imaging techniques to enhance our screening capabilities, allowing for real-time monitoring of ion channel activity in live cells.

We provide assays for different GABAA receptor subtypes (e.g., α1, α2, β2, γ2) to help you identify selective modulators for precise therapeutic targeting. Our assays can be customized to identify compounds that act as agonists (activators) or antagonists (inhibitors) of the GABAA receptor. For clients looking to screen large compound libraries for GABAA receptor activity, we offer high-throughput screening capabilities, allowing you to assess the pharmacological profiles of numerous compounds efficiently.

Applications

The GABAA channel assay can indeed be relevant for a diverse range of physiological and pharmacological areas, given its integral role in the functioning of the central nervous system. Our GABAA channel assay is versatile and applicable across various ion channel profiling, including:

• Pain-Inflammation Ion Channel Portfolio
• Seizure-Convulsion Ion Channel Portfolio
• Pulmonary-Respiratory Ion Channel Portfolio
• Psychiatric Disorder Ion Channel Portfolio
• Sedation Off Target Portfolio
• Depression Ion Channel Portfolio

Advantages

• Comprehensive and Customizable Assay Services
  Creative Biolabs offers fully customizable GABAA channel assays tailored to specific research needs. From receptor subtype selection to pharmacological screening, we provide precise and adaptable solutions that support both early discovery and advanced mechanistic studies across a broad range of therapeutic areas.
• Advanced Electrophysiological Techniques
  Our experienced electrophysiology team utilizes both automated and manual patch-clamp methods to deliver high-resolution, reproducible measurements of GABAA receptor function. These techniques are ideal for characterizing ion channel kinetics, drug modulation effects, and subtype-specific responses with exceptional accuracy.
• High-Throughput Screening Efficiency
  To accelerate drug discovery, we support large-scale compound screening with high-throughput formats. Our platform enables efficient pharmacological profiling of compound libraries against multiple GABAA subtypes, significantly reducing timelines while maintaining data integrity and quality.
• Broad Application Coverage
  Our GABAA channel assay services are applicable to a wide range of disease models, including epilepsy, anxiety, insomnia, depression, and respiratory disorders. The assay supports multiple ion channel portfolios, allowing researchers to evaluate off-target effects or therapeutic potential with confidence.

Reference

1. Popova, E. "Ionotropic GABA receptors and distal retinal ON and OFF responses." Scientifica 2014.1 (2014): 149187. Distributed under Open Access license CC BY 3.0, without modification.

For Research Use Only | Not For Clinical Use