An N-sulfonyl-polyamine that acts as a potent and more specific antagonist ofnMDA receptors expressed in Xenopus oocytes (IC50 = 310, 340nM in NR1/NR2A and NR1/NR2B, respectively). The inhibition appears to be voltage-dependent and is non-competitive with respect to glutamate and glycine. Exhibits about 50-fold greater selectivity over NR1/NR2C and NR1/NR2D receptors (IC50 = 16 and 13uM, respectively). Also shown to block c-AMP-dependent, calmodulin-activated phosphodiesterase (IC50 = 58uM) and diminishes the induction of ornithine decarboxylase. At higher concentration (~100uM) it is shown to reduce spontaneous epileptiform activity in mouse cortical slices. Solubility: DMSO Primary Target: NMDA Primary Target IC50: 0.31u Storage and Stability: May be stored at 4C. For long-term storage, aliquot and store at 4C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
Purity:
~97% (HPLC)
Form:
Supplied as a yellowish-white powder.
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