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GABA transporters (gamma-aminobutyric acid transporters) are a family of neurotransmitter / sodium symporters, belonging to the solute carrier 6 family. [ 1 ] [ 2 ] They are found in various regions of the brain in different cell types, such as neurons and astrocytes .
The GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory compound in the mature vertebrate central nervous system. There are two classes of GABA receptors: GABA A and GABA B .
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The ionotropic GABA A receptor protein complex is also the molecular target of the benzodiazepine class of tranquilizer drugs. Benzodiazepines do not bind to the same receptor site on the protein complex as does the endogenous ligand GABA (whose binding site is located between α- and β-subunits), but bind to distinct benzodiazepine binding sites situated at the interface between the α- and ...
There is evidence to suggest that GABA transporters are linked to epilepsy, affective disorders, and schizophrenia. But considering that GAT1 and GAT3 are expressed at far higher levels in brain tissue, it is likely that inhibition of these transporters will have a far greater anticonvulsant effect than inhibition of GAT2 [ 2 ] and BGT1.
Neurotransmitters are essential to the function of complex neural systems. The exact number of unique neurotransmitters in humans is unknown, but more than 100 have been identified. [3] Common neurotransmitters include glutamate, GABA, acetylcholine, glycine, dopamine and norepinephrine.
GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts on the repertoire of GABA A receptors, the ligand-gated chloride channels. It is assembled from a diverse subunit pool, including assemblies from a family of 19 subunits (α1-α6, β1-β3, γ1-γ3, δ, ∈, θ, π and ρ1-ρ3).
The stoichiometry for GABA Transporter 1 is 2 Na +: 1 Cl −: 1 GABA. [13] The presence of a Cl − /Cl − exchange is also proposed because the Cl − transported across the membrane does not affect the net charge. [14] GABA is also the primary inhibitory neurotransmitter in the cerebral cortex and has the highest level of expression within ...