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The **GABA\(_A\) receptor** is a major ionotropic receptor in the central nervous system that mediates fast synaptic inhibition via chloride ion influx upon activation by GABA, the principal inhibitory neurotransmitter. It is a pentameric protein composed of combinations of α, β, γ, δ, ε, π, θ, and ρ subunits, with structural and functional heterogeneity dictating pharmacological properties and regional distribution[1][2][4]. These receptors have multiple modulatory and allosteric sites that are the targets of various therapeutic drugs, especially benzodiazepines, barbiturates, and anesthetics, playing crucial roles in neurological and psychiatric conditions.
Positive allosteric modulators (increase frequency or duration of channel opening); Channel blockers (inhibit Cl\(⁻\) flow); Direct agonists (activate receptor); Antagonists (block GABA binding or allosteric sites)
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