product summary
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company name :
Tocris Bioscience
product type :
chemical
product name :
0111/1
catalog :
0111/1
quantity :
1 mg (also 10 mg, 50 mg)
price :
121 USD
more info or order :
citations: 18
Reference
Romanos J, Benke D, Saab A, Zeilhofer H, Santello M. Differences in glutamate uptake between cortical regions impact neuronal NMDA receptor activation. Commun Biol. 2019;2:127 pubmed publisher
Gasull Camós J, Martínez Torres S, Tarrés Gatius M, Ozaita A, Artigas F, Castañé A. Serotonergic mechanisms involved in antidepressant-like responses evoked by GLT-1 blockade in rat infralimbic cortex. Neuropharmacology. 2018;139:41-51 pubmed publisher
Pál I, Kardos J, Dobolyi Ã, Héja L. Appearance of fast astrocytic component in voltage-sensitive dye imaging of neural activity. Mol Brain. 2015;8:35 pubmed publisher
Petr G, Sun Y, Frederick N, Zhou Y, Dhamne S, Hameed M, et al. 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. 2015;35:5187-201 pubmed publisher
Campbell S, Hablitz J, Olsen M. Functional changes in glutamate transporters and astrocyte biophysical properties in a rodent model of focal cortical dysplasia. Front Cell Neurosci. 2014;8:425 pubmed publisher
Tse D, Chung I, Wu S. Pharmacological inhibitions of glutamate transporters EAAT1 and EAAT2 compromise glutamate transport in photoreceptor to ON-bipolar cell synapses. Vision Res. 2014;103:49-62 pubmed publisher
Liang J, Chao D, Sandhu H, Yu Y, Zhang L, Balboni G, et al. ?-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes. Br J Pharmacol. 2014;171:5417-30 pubmed publisher
Foran E, Rosenblum L, Bogush A, Pasinelli P, Trotti D. Sumoylation of the astroglial glutamate transporter EAAT2 governs its intracellular compartmentalization. Glia. 2014;62:1241-53 pubmed publisher
Okabe Y, Takahashi T, Mitsumasu C, Kosai K, Tanaka E, Matsuishi T. Alterations of gene expression and glutamate clearance in astrocytes derived from an MeCP2-null mouse model of Rett syndrome. PLoS ONE. 2012;7:e35354 pubmed publisher
Jiang E, Yan X, Weng H. Glial glutamate transporter and glutamine synthetase regulate GABAergic synaptic strength in the spinal dorsal horn. J Neurochem. 2012;121:526-36 pubmed publisher
McKeown K, Moreno R, Hall V, Ribera A, Downes G. Disruption of Eaat2b, a glutamate transporter, results in abnormal motor behaviors in developing zebrafish. Dev Biol. 2012;362:162-71 pubmed publisher
Hobo S, Eisenach J, Hayashida K. Up-regulation of spinal glutamate transporters contributes to anti-hypersensitive effects of valproate in rats after peripheral nerve injury. Neurosci Lett. 2011;502:52-5 pubmed publisher
Parri H, Gould T, Crunelli V. Sensory and cortical activation of distinct glial cell subtypes in the somatosensory thalamus of young rats. Eur J Neurosci. 2010;32:29-40 pubmed publisher
David Y, Cacheaux L, Ivens S, Lapilover E, Heinemann U, Kaufer D, et al. Astrocytic dysfunction in epileptogenesis: consequence of altered potassium and glutamate homeostasis?. J Neurosci. 2009;29:10588-99 pubmed publisher
Mulholland P, Carpenter Hyland E, Woodward J, Chandler L. Ethanol disrupts NMDA receptor and astroglial EAAT2 modulation of Kv2.1 potassium channels in hippocampus. Alcohol. 2009;43:45-50 pubmed publisher
Weller M, Stone I, Goss A, Rau T, Rova C, Poulsen D. Selective overexpression of excitatory amino acid transporter 2 (EAAT2) in astrocytes enhances neuroprotection from moderate but not severe hypoxia-ischemia. Neuroscience. 2008;155:1204-11 pubmed publisher
Baltan S, Besancon E, Mbow B, Ye Z, Hamner M, Ransom B. White matter vulnerability to ischemic injury increases with age because of enhanced excitotoxicity. J Neurosci. 2008;28:1479-89 pubmed publisher
Chu K, Lee S, Sinn D, Ko S, Kim E, Kim J, et al. Pharmacological Induction of Ischemic Tolerance by Glutamate Transporter-1 (EAAT2) Upregulation. Stroke. 2007;38:177-82 pubmed
product information
master code :
111
SKU :
0111/1
product name :
Dihydrokainic acid
unit size :
1 mg (also 10 mg, 50 mg)
description :
EAAT2 (GLT-1)-selective non-transportable inhibitor of L-glutamate and L-aspartate uptake
target :
Glutamate (EAAT) Transporter Inhibitors
category :
Small Molecules
observed molecular weight :
215.25
url print :
?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
Dihydrokainic acid is a selective EAAT2(GLT1) non-transportable inhibitor of L-glutamate and L-aspartate uptake (Ki = 23 u M). 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 M, 3 mM and 3 mM, respectively. Respective Km values in a FLIPR Membrane Potential (FMP) assay, are 31 M, 3 mM and 3 mM
top caption :
EAAT2 (GLT-1)-selective non-transportable inhibitor of L-glutamate and L-aspartate uptake
extended description :
EAAT2 (GLT-1)-selective non-transportable inhibitor of L-glutamate and L-aspartate uptake
chemical name text :
(2S,3S,4R)-2-Carboxy-4-isopropyl-3-pyrrolidineacetic acid
formula :
C10H17NO4
formula text :
C10H17NO4
cas num :
52497-36-6
USD :
121 USD
product details :
EAAT2 (GLT-1)-selective non-transportable inhibitor of L-glutamate and L-aspartate uptake
storage :
Store at RT
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK