GluN2D (formerly NR2D) antagonist, with some subunit selectivity
Biological descriptionGluN2D (formerly NR2D) antagonist, displaying modest GluN2 (NR2) subunit selectivity. Shows 7-fold selectivity for GluN2D (NR2D)-containing NMDA receptors vs. GluN2B (NR2B) and 5-fold selectivity over GluN2A (NR2A ) but does not discriminate between GluN2C (NR2C) and GluN2D (NR2D). Ki values are 22 (NR1/2A), 17.2 (NR1/2B), 5.24 (NR1/2C) and 2.36 μM (NR1/2D).
Chemical name(2R*,3S*)-1-(Phenanthrenyl-3-carbonyl)piperazine-2,3-dicarboxylic acid
Storage instructionsStore at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Solubility overviewSoluble in 2 eq. NaOH to 50 mM (with warming)
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Costa BM et al. N-methyl-D-aspartate (NMDA) receptor NR2 subunit selectivity of a series of novel piperazine-2,3-dicarboxylate derivatives: preferential blockade of extrasynaptic NMDA receptors in the rat hippocampal CA3-CA1 synapse. J Pharmacol Exp Ther331:618-26 (2009).
Read more (PubMed: 19684252) »
Brothwell SL et al. NR2B- and NR2D-containing synaptic NMDA receptors in developing rat substantia nigra pars compacta dopaminergic neurones. J Physiol586:739-50 (2008).
Read more (PubMed: 18033813) »
Morley RM et al. Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists. J Med Chem48:2627-37 (2005).
Read more (PubMed: 15801853) »