Biochem/physiol Actions

Primary TargetGluK1

Secondary TargetGluk3

General description

A potent antagonist highly selective for GluK1 (K_b = 10 nM), GluK3 (IC₅₀ = 23 nM), and GluK1/K5 (K_b = 8 nM) subtype kainate receptors. Does not interact with GluK2 and GluK2/K5 receptors. Low affinity to AMPA receptors (K_d = 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)