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The gamma-aminobutyric acid type A receptor (GABA_A receptor) is a pentameric ligand-gated chloride ion channel that mediates the majority of fast inhibitory neurotransmission in the central nervous system[1][2][3][9]. Each receptor is assembled from five subunits, typically including combinations of α, β, and γ subunits, giving rise to substantial functional diversity[1][2][9]. Upon binding GABA (the major CNS inhibitory neurotransmitter), the receptor opens a central chloride-conducting pore, leading to hyperpolarization of the neuron and neuronal inhibition[1][7][9]. GABA_A receptors are the principal pharmacological targets for clinically important drug classes such as benzodiazepines, barbiturates, and general anesthetics[6][9]. Dysfunction or altered expression is implicated in epilepsy, anxiety, sleep disorders, and several neurodevelopmental and psychiatric conditions[7][9]. Additional clarification: The provided query ("Central nervous system GABA receptor") is not the most precise name. The correct, canonical target is the GABA_A receptor, which mediates the fast synaptic inhibition in the CNS. There are other GABA receptors (notably GABA_B and GABA_C/ρ), so the input is ambiguous and is marked as "is_incorrect: true" to flag lack of specificity and nomenclature precision[5][7]. The abbreviation "GABA" alone does not refer to a receptor, but to the ligand (γ-aminobutyric acid). If you require information about metabotropic GABA_B receptors, separate this as a distinct query.
Positive allosteric modulation (e.g., benzodiazepines increase frequency of channel opening), Direct agonism (e.g., GABA, muscimol), Channel blockade (e.g., picrotoxin, inhibits channel function), Negative allosteric modulation (e.g., some convulsants).
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