A competitive, non-transportable blocker of excitatory amino acid transporters (IC50 values are 70, 6, and 6 μM for EAAT1, EAAT2 and EAAT3 respectively). Also inhibits EAAT4 and EAAT5 (Ki values are 4.4 and 3.2 μM respectively). Displays high selectivity for EAATs over ionotropic and metabotropic glutamate receptors. Also available as part of the Excitatory Amino Acid Transporter Inhibitor Tocriset™.
Sold for research purposes under license from Suntory Ltd.
|Storage||Desiccate at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|water||1.2||5mM with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 239.23. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||4.18 mL||20.9 mL||41.8 mL|
|5 mM||0.84 mL||4.18 mL||8.36 mL|
|10 mM||0.42 mL||2.09 mL||4.18 mL|
|50 mM||0.08 mL||0.42 mL||0.84 mL|
References are publications that support the products' biological activity.
Jabaudon et al (1999) Inhibition of uptake unmasks rapid extracellular turnover of glutamate of nonvesicular origin. Proc.Natl.Acad.Sci.U.S.A. 96 8733 PMID: 10411944
Shigeri et al (2001) Effects of threo-β-hydroxyaspartate derivatives on excitatory amino acid transporters (EAAT4 and EAAT5). J.Neurochem. 79 297 PMID: 11677257
Shimamoto et al (1998) DL-threo-β-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters. Mol.Pharmacol. 53 195 PMID: 9463476
Shimamoto et al (2000) Syntheses of optically pure β-hydroxyaspartate derivatives as glutamate transporter blockers. Bioorg.Med.Chem.Lett. 10 2407 PMID: 11078189
If you know of a relevant reference for DL-TBOA, please let us know.
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Keywords: DL-TBOA, supplier, non-transportable, inhibitors, inhibits, EAATs, EAAT1, EAAT2, EAAT3, EAAT4, EAAT5, Excitatory, Amino, Acid, Transporters, GLAST, GLT-1, Glutamate, Monoamine, Neurotransmitter, Glutamate, Transporters, Glutamate, Transporters, Tocris Bioscience
41 Citations for DL-TBOA
Citations are publications that use Tocris products. Selected citations for DL-TBOA include:
Wang et al (2012) Astrocytes modulate neural network activity by Ca2+-dependent uptake of extracellular K+. PLoS One 5 ra26 PMID: 22472648
Bender et al (2006) Two coincidence detectors for spike timing-dependent plasticity in somatosensory cortex. J Neurosci 26 4166 PMID: 16624937
Yang et al (2005) Behavioral stress enhances hippocampal CA1 long-term depression through the blockade of the glutamate uptake. Neuroscience 25 4288 PMID: 15858055
Armbruster et al (2014) Laser-scanning astrocyte mapping reveals increased glutamate-responsive domain size and disrupted maturation of glutamate uptake following neonatal cortical freeze-lesion. Front Cell Neurosci 8 277 PMID: 25249939
Zhou et al (2014) Cerebellar modules operate at different frequencies. Elife 3 e02536 PMID: 24843004
Mohr et al (2010) Young age and low temperature, but not female gender delay ATP loss and glutamate release, and protect Purkinje cells during simulated ischemia in cerebellar slices. Neuropharmacology 58 392 PMID: 19825379
Maurer et al (2010) Distinct retinal deficits in a zebrafish pyruvate dehydrogenase-deficient mutant. J Neurosci 30 11962 PMID: 20826660
Mulholland and Chandler (2010) Inhibition of glutamate transporters couples to Kv4.2 dephosphorylation through activation of extrasynaptic NMDA receptors. PLoS One 165 130 PMID: 19850106
Campbell et al (2015) Functional changes in glutamate transporters and astrocyte biophysical properties in a rodent model of focal cortical dysplasia. BMC Cancer 8 425 PMID: 25565960
Pedraz-Cuesta et al (2015) The glutamate transport inhibitor DL-Threo-β-Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells. J Neurosci 15 411 PMID: 25981639
Petr et al (2015) Conditional deletion of the glutamate transporter GLT-1 reveals that astrocytic GLT-1 protects against fatal epilepsy while neuronal GLT-1 contributes significantly to glutamate uptake into synaptosomes. Sci Rep 35 5187 PMID: 25834045
Kuebler et al (2015) Burst predicting neurons survive an in vitro glutamate injury model of cerebral ischemia. J Neurosci 5 17718 PMID: 26648112
Vance et al (2015) PAR1-activated astrocytes in the nucleus of the solitary tract stimulate adjacent neurons via NMDA receptors. J Neurosci 35 776 PMID: 25589770
Megill et al (2015) Defective Age-Dependent Metaplasticity in a Mouse Model of Alzheimer's Disease. Nat Protoc 35 11346 PMID: 26269641
Lin et al (2015) Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals. Elife 16 5555 PMID: 25768340
Rosa et al (2015) Neuron-glia signaling in developing retina mediated by neurotransmitter spillover. J Neurosci 4 PMID: 26274565
Huang et al (2015) Acidosis-Induced Dysfunction of Cortical GABAergic Neurons through Astrocyte-Related Excitotoxicity. Invest Ophthalmol Vis Sci 10 e0140324 PMID: 26474076
Romei et al (2016) Colocalization of neurotransmitter transporters on the plasma membrane of the same nerve terminal may reflect cotransmission. Brain Research Bulletin 127 100 PMID: 27565422
Ichinose and Lukasiewicz (2012) The mode of retinal presynaptic inhibition switches with light intensity. J Neurosci 32 4360 PMID: 22457487
Jarzylo and Man (2012) Parasynaptic NMDA receptor signaling couples neuronal glutamate transporter function to AMPA receptor synaptic distribution and stability. J Neurosci 32 2552 PMID: 22396428
Krock et al (2009) Retrograde intraflagellar transport by cytoplasmic dynein-2 is required for outer segment extension in vertebrate photoreceptors but not arrestin translocation. Invest Ophthalmol Vis Sci 50 5463 PMID: 19474410
Tovar-y-Romo et al (2013) Adenosine triphosphate released from HIV-infected macrophages regulates glutamatergic tone and dendritic spine density on neurons. J Neuroimmune Pharmacol 8 998 PMID: 23686368
Jeon et al (2013) Presynaptic Localization and Possible Function of Calcium-Activated Chloride Channel Anoctamin 1 in the Mammalian Retina. PLoS One 8 e67989 PMID: 23840801
Georgieva et al (2013) Conformational ensemble of the sodium-coupled aspartate transporter. Nat Struct Mol Biol 20 215 PMID: 23334289
Baltan et al (2008) White matter vulnerability to ischemic injury increases with age because of enhanced excitotoxicity. Br J Pharmacol 28 1479 PMID: 18256269
Falgairolle and O'Donovan (2015) Pharmacological Investigation of Fluoro-Gold Entry into Spinal Neurons. J Neurosci 10 e0131430 PMID: 26102354
Vandenberg et al (2011) Water and urea permeation pathways of the human excitatory amino acid transporter EAAT1. Biochem J 439 333 PMID: 21732909
Zou et al (2011) Morphine potentiates neurodegenerative effects of HIV-1 Tat through actions at μ-opioid receptor-expressing glia. Brain 134 3616 PMID: 22102648
Costa et al (2008) Electrophysiology and pharmacology of striatal neuronal dysfunction induced by mitochondrial complex I inhibition. J Neurosci 28 8040 PMID: 18685029
Léveillé et al (2008) Neuronal viability is controlled by a functional relation between synaptic and extrasynaptic NMDA receptors. FASEB J 22 4258 PMID: 18711223
Stridh et al (2008) Stimulated efflux of amino acids and glutathione from cultured hippocampal slices by omission of extracellular calcium: likely involvement of connexin hemichannels. J Biol Chem 283 10347 PMID: 18272524
Liang et al (2014) δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes. Vision Res 171 5417 PMID: 25052197
Tse et al (2014) Possible roles of glutamate transporter EAAT5 in mouse cone depolarizing bipolar cell light responses. Vision Res 103 63 PMID: 24972005
Tse et al (2014) Pharmacological inhibitions of glutamate transporters EAAT1 and EAAT2 compromise glutamate transport in photoreceptor to ON-bipolar cell synapses. J Neurophysiol 103 49 PMID: 25152321
McCall et al (2013) Fabrication and application of flexible, multimodal light-emitting devices for wireless optogenetics. Sci Signal 8 2413 PMID: 24202555
He et al (2013) Synaptic and extrasynaptic plasticity in glutamatergic circuits involving dentate granule cells following chronic N-methyl-D-aspartate receptor inhibition. Int J Mol Sci 109 1535 PMID: 23255721
Duguid et al (2007) Somatodendritic release of glutamate regulates synaptic inhibition in cerebellar Purkinje cells via autocrine mGluR1 activation. J Neurosci 27 12464 PMID: 18003824
Griffin et al (2015) Repeated cycles of chronic intermittent ethanol exposure increases basal glutamate in the nucleus accumbens of mice without affecting glutamate transport. Front Pharmacol 6 27 PMID: 25755641
Cengiz et al (2014) Sustained Na+/H+ exchanger activation promotes gliotransmitter release from reactive hippocampal astrocytes following oxygen-glucose deprivation. PLoS One 9 e84294 PMID: 24392123
Biase et al (2010) Excitability and synaptic communication within the oligodendrocyte lineage. Front Cell Neurosci 30 3600 PMID: 20219994
Matsui et al (2006) Effects of ethanol on photoreceptors and visual function in developing zebrafish. J Neurosci 47 4589 PMID: 17003456
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
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Huntington's Disease Poster
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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.