GABA_A Related Drug Discovery Products

The primary inhibitory neurotransmitter in the mammalian central nervous system (CNS) is γ-aminobutyric acid (GABA). Conducting ionotropic GABA_A receptors (GABA_ARs) and the slower-acting, G protein-coupled metabotropic GABA_B receptors (GABA_BRs) are the two types of receptors that GABA uses to exert its inhibitory effects. A few pieces of evidence highlight the fact that GABA_ARs play crucial physiological roles and are widely expressed throughout the mammalian CNS. Developmental abnormalities, sensory dysfunction, hypersensitive behavior, anxiety, epilepsy, and/or shorter lifespan are brought on by the mutation or deletion of several genes encoding GABA_AR subunits. Autism, schizophrenia, and a number of idiopathic epileptic disorders in humans have all been linked to aberrant GABA_AR trafficking, expression, and/or gating effects. Furthermore, genetic association studies have connected GABA_AR subunit genes to bipolar illnesses, autism, eating disorders, and alcoholism.

Creative Biolabs provides GABA_A related drug discovery tools to facilitate our customers' development of membrane protein drugs:

• GABA_A Assays
• Ion Channel Cell Lines
• Ion Channel Membranes
• Membrane Protein Tools

Overview of GABA_A

At least 19 GABA_AR subunit genes (α1–6, β1–3, γ1–3, δ, ε, θ, π, and ρ1–3) have been found in the human genome. The existence of a few dozen combinations in vivo, according to experimental data, shows that GABA_AR assembly is a selective process rather than a random one. Certain subunits are favoured over others to create dimeric intermediates that eventually assemble into pentameric complexes, according to a suggested hierarchical assembly mechanism. In heterologous cell cultures, the surface expression of fully functional pentameric receptors requires both the α and β subunits. It has been demonstrated that the third γ subunit increases the effectiveness of receptor assembly. Recombinant expression of the individual α, β, and γ subunits as well as the and combinations, on the other hand, mostly produced di-, tri-, and tetrameric oligomers that were kept in the endoplasmic reticulum. The homomeric β1 and β3 as well as the heteromeric β3γ2 receptors, however, are a few prominent exceptions that express well in heterologous systems.

GABA_A Drug Discovery

The identification of GABA_A receptor physiological and pharmacological functions has rekindled interest in the GABA_A receptor system as a target for the development of drugs with indications that are distinct from those of classical benzodiazepines and fewer side effects than those of those drugs. Today, a sizable number of drugs have been created that exhibit GABA_A receptor subtype selectivity by affinity, effectiveness, or both. Recent scientific advancements offer optimism for the development of analgesic pharmaceuticals for the treatment of chronic pain in addition to the development of non-sedative anxiolytics and cognition-improving medications.