GAT1 | GABA transporter subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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GAT1

Target not currently curated in GtoImmuPdb

Target id: 929

Nomenclature: GAT1

Systematic Nomenclature: SLC6A1

Family: GABA transporter subfamily

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 599 3p25.3 SLC6A1 solute carrier family 6 member 1
Mouse - 599 6 53.05 cM Slc6a1 solute carrier family 6 (neurotransmitter transporter
Rat - 599 4q42 Slc6a1 solute carrier family 6 member 1
Previous and Unofficial Names
GAT-A | GABATR | GABA transporter protein | Gabt1 | sodium- and chloride-dependent GABA transporter 1 | Gabt | XT-1 | Xtrp1 | GABATHG | solute carrier family 6 (neurotransmitter transporter), member 1 | solute carrier family 6 (neurotransmitter transporter
Database Links
Specialist databases
Bioparadigms SLC Tables SLC6A1 (Hs)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
UniProtKB
Wikipedia
Substrates and Reaction Kinetics
Substrate Sp. Property Value Units Standard property Standard value Assay description Assay conditions Comments Reference
GABA Hs -
nipecotic acid Hs -
guvacine Hs -
Stoichiometry
2Na+: 1Cl-: 1GABA

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
NNC-711 Hs Inhibition 7.4 pIC50 1
pIC50 7.4 (IC50 4x10-8 M) [1]
tiagabine Hs Inhibition 7.2 pIC50 1
pIC50 7.2 (IC50 7x10-8 M) [1]
SKF89976A Hs Inhibition 6.9 pIC50 2
pIC50 6.9 (IC50 1.3x10-7 M) [2]
CI-966 Hs Inhibition 6.6 pIC50 1
pIC50 6.6 (IC50 2.6x10-7 M) [1]
LU32-176B Mm Inhibition 5.4 pIC50 3
pIC50 5.4 (IC50 4x10-6 M) [3]
(R/S) EF-1500 Hs Inhibition 4.9 – 5.7 pIC50
pIC50 4.9 – 5.7 (IC50 1.3x10-5 – 2x10-6 M)
(R)-EF-1520 Hs Inhibition 5.1 – 5.4 pIC50
pIC50 5.1 – 5.4 (IC50 8.9x10-6 – 4x10-6 M)
(S)-EF-1520 Hs Inhibition 3.6 – 3.9 pIC50
pIC50 3.6 – 3.9 (IC50 2.5x10-4 – 1.2x10-4 M)
[3H]tiagabine Hs Inhibition - -
View species-specific inhibitor tables

References

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1. Borden LA, Murali Dhar TG, Smith KE, Weinshank RL, Branchek TA, Gluchowski C. (1994) Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur. J. Pharmacol., 269 (2): 219-24. [PMID:7851497]

2. Dhar TGM, Nakanishi H, Borden LA, Gluchowski C. (1996) On the bioactive conformation of the GABA uptake inhibitor SK&F 89976-A. Bioorg. Med. Chem. Lett., 6 (13): 1535 -1540.

3. White HS, Watson WP, Hansen SL, Slough S, Perregaard J, Sarup A, Bolvig T, Petersen G, Larsson OM, Clausen RP et al.. (2005) First demonstration of a functional role for central nervous system betaine/{gamma}-aminobutyric acid transporter (mGAT2) based on synergistic anticonvulsant action among inhibitors of mGAT1 and mGAT2. J. Pharmacol. Exp. Ther., 312 (2): 866-74. [PMID:15550575]

Contributors

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