Dihydrokainic acid

Catalog #: 0111
16 Citations Datasheet / COA / SDS

Catalog #	Availability	Size / Price	Qty
0111/1
0111/10
0111/50

Dihydrokainic acid | CAS No. 52497-36-6 | Glutamate (EAAT) Transporter Inhibitors

1 Image

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

View All Products for Glutamate (EAAT) Transporter Inhibitors

Product Details

Citations (16)

Supplemental Products

Reviews

Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

Dihydrokainic acid is a selective EAAT2(GLT1) non-transportable inhibitor of L-glutamate and L-aspartate uptake (K_i = 23 μM). Dihydrokainic acid is 130-fold selective over EAAT1 and EAAT3 (K_i > 3 mM). In [³H]-d-Asp uptake assays in HEK293 cells expressing human EAAT2, EAAT1 and EAAT3, K_i values are 89 μM, > 3 mM and > 3 mM, respectively. Respective K_m values in a FLIPR Membrane Potential (FMP) assay, are 31 μM, > 3 mM and > 3 mM

Technical 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

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

Product Datasheets

COA view current batch

Or select another batch:

View Batch

SDS

Reconstitution Calculator

Molarity Calculator

Reconstitution Calculator

Molarity Calculator

Mass

Concentration

Volume

M. Wt* g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

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

Differences in glutamate uptake between cortical regions impact neuronal NMDA receptor activation.
Authors: Romanos Et al.
Commun Biol 2019;2:127
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
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
Appearance of fast astrocytic component in voltage-sensitive dye imaging of neural activity.
Authors: Pál Et al.
Mol Brain 2015;8:35
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
Sumoylation of the astroglial glutamate transporter EAAT2 governs its intracellular compartmentalization.
Authors: Foran Et al.
Glia 2014;62:1241
δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes.
Authors: Liang Et al.
Br J Pharmacol 2014;171:5417
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
Disruption of Eaat2b, a glutamate transporter, results in abnormal motor behaviors in developing zebrafish.
Authors: McKeown Et al.
Dev Biol 2012;362:162
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

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

Ethanol disrupts NMDA receptor and astroglial EAAT2 modulation of Kv2.1 potassium channels in hippocampus.
Authors: Mulholland Et al.
Alcohol 2009;43:45

Astrocytic dysfunction in epileptogenesis: consequence of altered potassium and glutamate homeostasis?
Authors: David Et al.
J Neurosci 2009;29:10588

White matter vulnerability to ischemic injury increases with age because of enhanced excitotoxicity.
Authors: Baltan Et al.
J Neurosci 2008;28:1479

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

Pharmacological Induction of Ischemic Tolerance by Glutamate Transporter-1 (EAAT2) Upregulation.
Authors: Chu Et al.
Stroke 2007;38:177

FAQs

No product specific FAQs exist for this product, however you may

View all Small Molecule FAQs

Reviews for Dihydrokainic acid

There are currently no reviews for this product. Be the first to review Dihydrokainic acid and earn rewards!

Have you used Dihydrokainic acid?

Submit a review and receive an Amazon gift card.

$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.