A class of biologically active peptide molecules that interact with the GABAergic system, primarily by modulating the activity of Gamma-Aminobutyric Acid (GABA) receptors in the central nervous system. GABA is the principal inhibitory neurotransmitter, and these peptides function to promote anxiolysis, sedation, and neuronal balance by enhancing inhibitory signaling. They play a critical role in regulating mood and stress responses.
Origin
The term is a compound of GABAergic, referring to any substance that affects GABA, and peptide, indicating a short chain of amino acids. These molecules are identified through neurochemical research, often isolated from natural sources or synthesized as therapeutic agents. Their study belongs to the specialized domain of neuropeptidomics and psychopharmacology.
Mechanism
These peptides typically function as allosteric modulators, binding to a site on the GABA-A receptor distinct from the primary GABA binding site. This binding event alters the receptor’s conformation, increasing the frequency or duration of the chloride ion channel opening when GABA is present. The resulting influx of negative chloride ions hyperpolarizes the neuron, thereby decreasing its excitability and promoting a state of calm and reduced anxiety.
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