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GABA transporter subfamily C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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The activity of GABA-transporters located predominantly upon neurones (GAT-1), glia (GAT-3) or both (GAT-2, BGT-1) serves to terminate phasic GABA-ergic transmission, maintain low ambient extracellular concentrations of GABA, and recycle GABA for reuse by neurones. Nonetheless, ambient concentrations of GABA are sufficient to sustain tonic inhibition mediated by high affinity GABAA receptors in certain neuronal populations [18]. GAT1 is the predominant GABA transporter in the brain and occurs primarily upon the terminals of presynaptic neurones and to a much lesser extent upon distal astocytic processes that are in proximity to axons terminals. GAT3 resides predominantly on distal astrocytic terminals that are close to the GABAergic synapse. By contrast, BGT1 occupies an extrasynaptic location possibly along with GAT2 which has limited expression in the brain [15]. TauT is a high affinity taurine transporter involved in osmotic balance that occurs in the brain and non-neuronal tissues, such as the kidney, brush border membrane of the intestine and blood brain barrier [4,12]. CT1, which transports creatine, has a ubiquitous expression pattern, often co-localizing with creatine kinase [4].

Transporters

932
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GAT1 / SLC6A1 C Show summary » More detailed page go icon to follow link

GAT2 / SLC6A13 C Show summary »

GAT3 / SLC6A11 C Show summary »

BGT1 / SLC6A12 C Show summary »


Target Id 932
Nomenclature BGT1
Systematic nomenclature SLC6A12
Previous and unofficial names Betaine/GABA transporter 1 | GABA transporter 1 | Gat1 | Na(+)/Cl(-) betaine/GABA transporter | sodium- and chloride-dependent betaine transporter | vesicular GABA transporter | VGAT | Gabt2 | GAT2 | solute carrier family 6 (neurotransmitter transporter, betaine/GABA), member 12 | solute carrier family 6 (neurotransmitter transporter), member 12 | solute carrier family 6 (neurotransmitter transporter
Genes SLC6A12 (Hs), Slc6a12 (Mm), Slc6a12 (Rn)
Ensembl ID ENSG00000111181 (Hs), ENSMUSG00000030109 (Mm), ENSRNOG00000013547 (Rn)
UniProtKB AC P48065 (Hs), P31651 (Mm), P48056 (Rn)
Bioparadigms SLC Tables SLC6A12 (Hs)
RESOLUTE SLC6A12 (Hs)
Endogenous substrates
GABA
betaine
Selective inhibitors
NNC052090 pKi 5.9 [19] - Mouse
(R/S) EF-1500 pIC50 4.9
(R)-EF-1520 pIC50 3.7 – 4.7
(S)-EF-1520 pIC50 3.6 – 4.5
LU32-176B pIC50 4.0 [20] - Mouse
Stoichiometry 3Na+: 1 (or 2) Cl-: 1GABA

TauT / SLC6A6 C Show summary »

CT1 / SLC6A8 C Show summary »

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References

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation (select format):

Concise Guide to PHARMACOLOGY citation:

Alexander SP, Kelly E, Mathie A, Peters JA, Veale EL et al. (2021) THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Transporters. Br J Pharmacol. 178 Suppl 1:S412-S513.