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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 ...
The signal is terminated by removal of GABA from the synaptic cleft by transport of GABA back into the nerve terminal by the plasma membrane GABA transporter (GAT) 1. GABA transporters in the plasma membrane help in regulating the concentration of GABA in the extracellular matrix by reabsorbing the transmitter and clearing the synapse.
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Tiagabine, a drug used as an anticonvulsant, acts by inhibiting the GABA transporter 1. Neurotransmitter transporters inhibitors Vesicular transporters could provide an alternative therapeutic target for the modulation of chemical neurotransmission, as the activity of these transporters could affect the quantity of neurotransmitter released.
Sodium- and chloride-dependent betaine transporter, also known as Na(+)/Cl(-) betaine/GABA transporter (BGT-1), is a protein that in humans is encoded by the SLC6A12 gene. BGT-1 is predominantly expressed in the liver (hepatocytes). [5] It is also expressed in the kidney [5] where it is regulated by NFAT5 during a response to osmotic stress. [6]
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.
The gamma-aminobutyric acid A receptor (GABA A receptor) is a multisubunit chloride channel that mediates the fastest inhibitory synaptic transmission in the central nervous system. This gene encodes GABA A receptor, beta 1 subunit. It is mapped to chromosome 4p12 in a cluster of genes encoding alpha 4, alpha 2 and gamma 1 subunits of the GABA ...
Vesicular inhibitory amino acid transporter is a protein that in humans is encoded by the SLC32A1 gene. [5] The protein encoded by this gene is an integral membrane protein involved in gamma-aminobutyric acid (GABA) and glycine uptake into synaptic vesicles. The encoded protein is a member of amino acid/polyamine transporter family II. [5]