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Glutamate (EAAT) Transporters

Glutamate transporters, also known as excitatory amino acid transporters (EAATs), are sodium- and potassium-dependent members of the solute carrier family 6 (SLC1), widely distributed throughout the brain. There are five EAAT subtypes, each with a specific distribution.

Products
Background
Literature (3)
Gene Data

Glutamate Transporter Modulators
Cat. No. Product Name / Activity
6578 GT 949
Potent and selective positive allosteric modulator of EAAT2

Glutamate Transporter Inhibitors
Cat. No. Product Name / Activity
0846 Chicago Sky Blue 6B
Potent inhibitor of L-glutamate uptake into synaptic vesicles; also inhibits MIF
3697 7-Chlorokynurenic acid sodium salt
Potent competitive inhibitor of L-glutamate uptake. Sodium salt of 7-Chlorokynurenic acid (Cat. No. 0237)
0237 7-Chlorokynurenic acid
Potent competitive inhibitor of L-glutamate uptake
0111 Dihydrokainic acid
EAAT2 (GLT-1)-selective non-transportable inhibitor of L-glutamate and L-aspartate uptake
0845 Evans Blue tetrasodium salt
Potent inhibitor of L-glutamate uptake into synaptic vesicles; also non-NMDA iGluR antagonist; P2X antagonist
0183 L-(-)-threo-3-Hydroxyaspartic acid
Transportable EAAT1-4 inhibitor/non-transportable EAAT5 inhibitor
0298 L-trans-2,4-PDC
Transportable EAAT1-4 inhibitor/non-transportable EAAT5 inhibitor
1223 DL-TBOA
Selective non-transportable inhibitor of EAATs
2532 TFB-TBOA
High affinity EAAT1 and EAAT2 blocker
3490 UCPH 101
Selective non-substrate EAAT1 inhibitor
2652 WAY 213613
Potent, non-substrate EAAT2 inhibitor

Related Targets

Glutamate transporters, also known as excitatory amino acid transporters (EAATs), are sodium- and potassium-dependent members of the solute carrier family 6 (SLC1) found widely distributed throughout the brain. There are five EAAT subtypes, each with a specific primary distribution; EAAT1 (cerebellar glia), EAAT2 (forebrain glia), EAAT3 (cortical neurons), EAAT4 (cerebellar Purkinje neurons) and EAAT5 (retina).

Functions of glutamate transporters include regulation of excitatory neurotransmission, maintenance of low ambient extracellular glutamate concentrations (protects against neurotoxicity) and providing glutamate for metabolism through the glutamate-glutamine cycle.

Overactivity of glutamate transporters has been implicated in the pathophysiology of schizophrenia and other mental illnesses, whilst underactivity is seen in ischemia and traumatic brain injury.

External sources of pharmacological information for Glutamate (EAAT) Transporters :

Literature for Glutamate (EAAT) Transporters

Tocris offers the following scientific literature for Glutamate (EAAT) Transporters to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Epilepsy Poster

Epilepsy Poster

Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.

Huntington's Disease Poster

Huntington's Disease Poster

Huntington's disease (HD) is a severe monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the effects of mutant huntingtin aggregation implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.

Schizophrenia Poster

Schizophrenia Poster

Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.

Glutamate Transporter Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
EAAT1 Human SLC1A3 NM_004172 P43003
Mouse Slc1a3 NM_148938 P56564
Rat Slc1a3 NM_019225 P24942
EAAT2 Human SLC1A2 NM_004171 P43004
Mouse Slc1a2 NM_001077514 P43006
Rat Slc1a2 NM_017215 Q91ZA9
EAAT3 Human SLC1A1 NM_004170 P43005
Mouse Slc1a1 NM_009199 P51906
Rat Slc1a1 NM_013032 P51907
EAAT4 Human SLC1A6 NM_005071 P48664
Mouse Slc1a6 NM_009200 O35544
Rat Slc1a6 NM_032065 O35921
EAAT5 Human SLC1A7 NM_006671 O00341
Mouse Slc1a7 NM_146255 Q8JZR4
Rat Slc1a7 NM_001108973 XP_345560

Properties of Glutamate Transporters

Subtype EAAT1 EAAT2 EAAT3 EAAT4 EAAT5
Primary Distribution Cerebellar glia Forebrain glia Cortical neurons Cerebellar Purkinje neurons Retina
Selected Inhibitors Ki (μM)
cis-ACBD (0271)1 170 680 230 - -
Dihydrokainic acid (0111) > 30002 232 > 30002 - -
L-(-)-threo-3-Hydroxyaspartic acid (0183)1 11 19 14 - -
(±)-threo-3-Methylglutamic acid (0811) 1600 (IC50)3 90 (IC50)3 1080 (IC50)3 109 (IC50)3 -
L-trans-2,4-PDC (0298) 791 81 611 - -
DL-TBOA (1223) 70 (IC50)4 6 (IC50)4 6 (IC50)4 4.45 3.25

References

  1. Jensen and Bauner-Osborne (2004) Pharmacological characterization of human excitatory amino acid transporters EAAT1, EAAT2 and EAAT3 in a fluorescense-based membrane potential assay. Biochem.Pharmacol. 67 2115.
  2. Arriza et al (1994) Functional comparisons of three glutamate transporter subtypes cloned from human motor cortex. J.Neurosci. 14 5559.
  3. Eliasof et al (2001) Pharmacological characterization of threo-3-methylglutamic acid with excitatory amino acid transporters in native and recombinant systems. J.Neurochem. 77 550.
  4. Jabaudon et al (1999) Inhibition of uptake unmasks rapid extracellular turnover of glutamate of nonvesicular origin. Proc.Natl.Acad.Sci.USA 96 8733.
  5. Shigeri et al (2001) Effects of threo-β-hydroxyaspartate derivatives on excitatory amino acid transporters (EAAT4 and EAAT5). J.Neurochem. 79 298.