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The GABA receptors are a class of receptors that respond to the neurotransmitter gamma ... GABA receptors influence neural function by coordinating with glutamatergic ...
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 ...
GABA is also the primary inhibitory neurotransmitter in the cerebral cortex and has the highest level of expression within it. [15] The GABA affinity (K m) of the mouse isoform of GAT1 is 8 μM. [16] In the brain of a mature mammal, glutamate is converted to GABA by the enzyme glutamate decarboxylase (GAD) along with the addition of vitamin B6.
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.
In pharmacology, GABA A receptor positive allosteric modulators, also known as GABAkines or GABA A receptor potentiators, [1] are positive allosteric modulator (PAM) molecules that increase the activity of the GABA A receptor protein in the vertebrate central nervous system. GABA is a major inhibitory neurotransmitter in the central nervous system.
In the mammalian brain, two predominant, differentially expressed isoforms of the GABA B1 are transcribed from the Gabbr1 gene, GABA B(1a) and GABA B(1b), which are conserved in different species including humans. [12] This might potentially offer more complexity in terms of the function due to different composition of the receptor. [12]
GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts at GABA-A receptors, which are ligand-gated chloride channels. Chloride conductance of these channels can be modulated by agents such as benzodiazepines that bind to the GABA-A receptor. At least 16 distinct subunits of GABA-A receptors have been identified. [6]
GABA-A has a pentametric form, with two alpha, two beta, and one gamma subunit. [6] The various subunit isoforms seen in the GABA-A receptor structure have an effect on its function. GABRA2 is most often seen as part of the most common expression α2β3γ2, which is seen in 13% of all GABA-A receptors. [7]