GABA receptors are a class of ligand-gated ion channels and G-protein coupled receptors found in the central nervous system that respond to the neurotransmitter Gamma-Aminobutyric Acid (GABA). GABA is the principal inhibitory neurotransmitter in the mature brain, and its receptors play a critical role in reducing neuronal excitability, thereby promoting relaxation, sedation, and anxiety reduction. These receptors are essential modulators of sleep cycles and emotional regulation.
Origin
The term combines the abbreviation for Gamma-Aminobutyric Acid with the general biological term ‘receptor,’ which denotes a protein molecule that receives chemical signals from outside the cell. The discovery of GABA as a key inhibitory neurotransmitter and the subsequent identification of its receptors occurred in the mid-20th century, foundational to modern neuropharmacology. This understanding is central to the treatment of anxiety and seizure disorders.
Mechanism
When GABA binds to its primary receptor subtype, the GABA-A receptor, it causes a conformational change that opens an intrinsic chloride ion channel. The influx of negatively charged chloride ions hyperpolarizes the neuron’s membrane, making it less likely to fire an action potential. This inhibitory mechanism dampens excessive neural activity throughout the brain, effectively calming the nervous system and is influenced by neurosteroids like allopregnanolone, which act as positive allosteric modulators.
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