A potent antagonist highly selective for GluK1 (Kb = 10 nM), GluK3 (IC50 = 23 nM), and GluK1/K5 (Kb = 8 nM) subtype kainate receptors. Does not interact with GluK2 and GluK2/K5 receptors. Low affinity to AMPA receptors (Kd = 83 µM). Does not interact with mGluR1 or NMDA receptors at concentration less than 10 µM. Often used in studying neuronal excitability and synaptic plasticity.
Biochem/physiol Actions
Primary Target GluK1
Secondary Target Gluk3
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Pinheiro, S., et al. 2013. Cereb. Cort.23, 323. Atlason, T., et al. 2010. Mol. Pharmacol.78, 1036. Perrais, D., et al. 2009. Neuropharmacol.56, 131. Dolman, P., et al. 2007. J. Med. Chem.50, 1558. Mayer, L., et al. 2006. J. Neurosci.26, 2852.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 2
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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