Dihydrokainic acid
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Description: EAAT2 (GLT-1)-selective non-transportable inhibitor of L-glutamate and L-aspartate uptake
Chemical Name: (2S,3S,4R)-2-Carboxy-4-isopropyl-3-pyrrolidineacetic acid
Biological Activity
Dihydrokainic acid is a selective EAAT2(GLT1) non-transportable inhibitor of L-glutamate and L-aspartate uptake (Ki = 23 μM). Dihydrokainic acid is 130-fold selective over EAAT1 and EAAT3 (Ki > 3 mM). In [3H]-d-Asp uptake assays in HEK293 cells expressing human EAAT2, EAAT1 and EAAT3, Ki values are 89 μM, > 3 mM and > 3 mM, respectively. Respective Km values in a FLIPR Membrane Potential (FMP) assay, are 31 μM, > 3 mM and > 3 mMTechnical Data
M.Wt:
215.25
Formula:
C10H17NO4
Solubility:
Soluble to 25 mM in water
Storage:
Store at RT
CAS No:
52497-36-6
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Glial glutamate transporter and glutamine synthetase regulate GABAergic synaptic strength in the spinal dorsal horn.
Jiang E, Yan X, Weng HR
J. Neurochem., 2012;121(4):526-36. -
Alterations of gene expression and glutamate clearance in astrocytes derived from an MeCP2-null mouse model of Rett syndrome.
Okabe Y, Takahashi T, Mitsumasu C, Kosai K, Tanaka E, Matsuishi T
PLoS ONE, 2012;7(4):e35354. -
Functional comparisons of three glutamate transporter subtypes cloned from human motor cortex.
Arriza et al.
J.Neurosci., 1994;14:5559 -
The neuronal and epithelial high affinity glutamate transporter, insights into structure and mechanism of transport.
Kanal et al.
J.Biol.Chem., 1994;269:20599 -
Effects of dihydrokainic acid on extracellular amino acids and neuronal excitability in the in vivo rat hippocampus.
Munoz et al.
Neuropharmacology, 1987;26:1 -
Pharmacological characterization of human excitatory amino acid transporters EAAT1, EAAT2 and EAAT3 in a fluorescence-based membrane potential assay.
Jensen and Bräuner-Osborne et al.
Biochem.Pharmacol., 2004;67:2115
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Citations for Dihydrokainic acid
The citations listed below are publications that use Tocris products. Selected citations for Dihydrokainic acid include:
16 Citations: Showing 1 - 10
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Differences in glutamate uptake between cortical regions impact neuronal NMDA receptor activation.
Authors: Romanos Et al.
Commun Biol 2019;2:127
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Serotonergic mechanisms involved in antidepressant-like responses evoked by GLT-1 blockade in rat infralimbic cortex.
Authors: Gasull-Camôs Et al.
Neuropharmacology 2018;139:41
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Functional changes in glutamate transporters and astrocyte biophysical properties in a rodent model of focal cortical dysplasia.
Authors: Campbell Et al.
Front Cell Neurosci 2015;8:425
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Appearance of fast astrocytic component in voltage-sensitive dye imaging of neural activity.
Authors: Pál Et al.
Mol Brain 2015;8:35
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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.
Authors: Petr Et al.
J Neurosci 2015;35:5187
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Sumoylation of the astroglial glutamate transporter EAAT2 governs its intracellular compartmentalization.
Authors: Foran Et al.
Glia 2014;62:1241
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δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes.
Authors: Liang Et al.
Br J Pharmacol 2014;171:5417
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Pharmacological inhibitions of glutamate transporters EAAT1 and EAAT2 compromise glutamate transport in photoreceptor to ON-bipolar cell synapses.
Authors: Tse Et al.
Vision Res 2014;103:49
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Disruption of Eaat2b, a glutamate transporter, results in abnormal motor behaviors in developing zebrafish.
Authors: McKeown Et al.
Dev Biol 2012;362:162
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Up-regulation of spinal glutamate transporters contributes to anti-hypersensitive effects of valproate in rats after peripheral nerve injury.
Authors: Hobo Et al.
Neurosci Lett 2011;502:52
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Sensory and cortical activation of distinct glial cell subtypes in the somatosensory thalamus of young rats.
Authors: Parri Et al.
Eur J Neurosci 2010;32:29
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Ethanol disrupts NMDA receptor and astroglial EAAT2 modulation of Kv2.1 potassium channels in hippocampus.
Authors: Mulholland Et al.
Alcohol 2009;43:45
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Astrocytic dysfunction in epileptogenesis: consequence of altered potassium and glutamate homeostasis?
Authors: David Et al.
J Neurosci 2009;29:10588
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White matter vulnerability to ischemic injury increases with age because of enhanced excitotoxicity.
Authors: Baltan Et al.
J Neurosci 2008;28:1479
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Selective overexpression of excitatory amino acid transporter 2 (EAAT2) in astrocytes enhances neuroprotection from moderate but not severe hypoxia-ischemia.
Authors: Weller Et al.
Neuroscience 2008;155:1204
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Pharmacological Induction of Ischemic Tolerance by Glutamate Transporter-1 (EAAT2) Upregulation.
Authors: Chu Et al.
Stroke 2007;38:177
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