Cat. No. 0111
Chemical Name: (2S,3S,4R)-2-Carboxy-4-isopropyl-3-
Biological ActivityEAAT2(GLT1)-selective non-transportable inhibitor of L-glutamate and L-aspartate uptake (Ki = 23 μM). 130-fold selective over EAAT1 and EAAT3 (Ki > 3 mM). Also available as part of the Excitatory Amino Acid Transporter Inhibitor Tocriset™.
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.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Arriza et al (1994) Functional comparisons of three glutamate transporter subtypes cloned from human motor cortex. J.Neurosci. 14 5559. PMID: 7521911.
Kanal et al (1994) The neuronal and epithelial high affinity glutamate transporter, insights into structure and mechanism of transport. J.Biol.Chem. 269 20599. PMID: 7914198.
Munoz et al (1987) Effects of dihydrokainic acid on extracellular amino acids and neuronal excitability in the in vivo rat hippocampus. Neuropharmacology 26 1. PMID: 2882438.
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Citations are publications that use Tocris products. Selected citations for Dihydrokainic acid include:
Campbell et al (2015) Functional changes in glutamate transporters and astrocyte biophysical properties in a rodent model of focal cortical dysplasia. Front Cell Neurosci 8 425. PMID: 25565960.
Pál et al (2015) Appearance of fast astrocytic component in voltage-sensitive dye imaging of neural activity. Mol Brain 8 35. PMID: 26043770.
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. J Neurosci 35 5187. PMID: 25834045.
Liang et al (2014) δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes. Br J Pharmacol 171 5417. PMID: 25052197.
Tse et al (2014) Pharmacological inhibitions of glutamate transporters EAAT1 and EAAT2 compromise glutamate transport in photoreceptor to ON-bipolar cell synapses. Vision Res 103 49. PMID: 25152321.
McKeown et al (2012) Disruption of Eaat2b, a glutamate transporter, results in abnormal motor behaviors in developing zebrafish. Dev Biol 362 162. PMID: 22094018.
Hobo et al (2011) Up-regulation of spinal glutamate transporters contributes to anti-hypersensitive effects of valproate in rats after peripheral nerve injury. Neurosci Lett 502 52. PMID: 21802494.
Parri et al (2010) Sensory and cortical activation of distinct glial cell subtypes in the somatosensory thalamus of young rats. Eur J Neurosci 32 29. PMID: 20608967.
David et al (2009) Astrocytic dysfunction in epileptogenesis: consequence of altered potassium and glutamate homeostasis? J Neurosci 29 10588. PMID: 19710312.
Mulholland et al (2009) Ethanol disrupts NMDA receptor and astroglial EAAT2 modulation of Kv2.1 potassium channels in hippocampus. Alcohol 43 45. PMID: 19185209.
Baltan et al (2008) White matter vulnerability to ischemic injury increases with age because of enhanced excitotoxicity. J Neurosci 28 1479. PMID: 18256269.
Weller et al (2008) Selective overexpression of excitatory amino acid transporter 2 (EAAT2) in astrocytes enhances neuroprotection from moderate but not severe hypoxia-ischemia. Neuroscience 155 1204. PMID: 18620031.
Chu et al (2007) Pharmacological Induction of Ischemic Tolerance by Glutamate Transporter-1 (EAAT2) Upregulation. Stroke 38 177. PMID: 17122424.
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Keywords: Dihydrokainic acid, supplier, EAAT2, GLT-1-selective, non-transportable, inhibitors, inhibits, L-glutamate, L-aspartate, uptake, Excitatory, Amino, Acid, Transporters, Monoamine, Neurotransmitter, Tocris Bioscience, Glutamate Transporter Inhibitor products
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