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
Gene Data

Inhibitors

Cat No Product Name / Activity
0271 cis-ACBD
Potent, selective L-glutamate uptake inhibitor
0332 L-CCG-lll
Potent, competitive glutamate uptake inhibitor
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
2217 (±)-HIP-A
Potent, non-competitive EAAT inhibitor
2218 (±)-HIP-B
Potent, non-competitive EAAT inhibitor
0183 L-(-)-threo-3-Hydroxyaspartic acid
Transportable EAAT1-4 inhibitor/non-transportable EAAT5 inhibitor
0811 (±)-threo-3-Methylglutamic acid
EAAT2 and EAAT4 blocker
0973 MPDC
Potent inhibitor of L-glutamate uptake. Less activity as a substrate compared to its parent compound, L-trans-2,4-PDC (Cat. No. 0298)
0298 L-trans-2,4-PDC
Transportable EAAT1-4 inhibitor/non-transportable EAAT5 inhibitor
0903 SYM 2081
Inhibits EAAT2. Also kainate receptor agonist
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

Other

Cat No Product Name / Activity
3732 Ceftriaxone disodium salt
Neuroprotective; increases EAAT2 expression and activity
5082 LDN 212320
Increases EAAT2 expression; neuroprotective
2277 MNI-caged-D-aspartate
Caged D-aspartate; EAAT substrate

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

    Neurodegeneration

    Neurodegeneration Product Guide

    A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:

    • Alzheimer's disease
    • Parkinson's disease
    • Huntington's disease
    Huntington's Disease

    Huntington's Disease Poster

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

    Schizophrenia

    Schizophrenia Poster

    Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster highlights the targets and pathways representing the most promising strategies to pursue for novel drug development.

    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.