NMDA Antagonist XI, N1-dansyl-spermine-Calbiochem

C₂₂H₃₇N₅O₂S · 3HCl

545.01

An N-sulfonyl-polyamine that acts as a potent and more specific antagonist of NMDA receptors expressed in Xenopus oocytes (IC₅₀ = 310, 340 nM 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 13 µM, respectively). Also shown to block c-AMP-dependent, calmodulin-activated phosphodiesterase (IC₅₀ = 58 µM) and diminishes the induction of ornithine decarboxylase. At higher concentration (˜100 µM) it is shown to reduce spontaneous epileptiform activity in mouse cortical slices.

Primary Target
NMDA

Toxicity: Standard Handling (A)

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

Kirby, B.P., et al. 2005, Eur. J. Pharmacol. 524, 53.
Li, J., et al. 2005, Brain Res. 1055, 180.
Kirby, B. et al. 2004, Brain Res. 1011, 69.
Seiler, N., et al. 1998, J. Biochem. Cell Biol. 30, 393.

Chao, J., et al. 1997, Mol. Pharm. 51, 861.

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

100

≥97% (HPLC)

powder

0.31 μM IC₅₀

Calbiochem^®

OK to freeze
protect from light

yellow-white

DMSO: 100 mg/mL

2-8℃

Packaged under inert gas

11 - Combustible Solids

WGK 3