5.05764

NMDA Antagonist XI, N1-dansyl-spermine

• Sinonimo/i: NMDA Antagonist XI, N1-dansyl-spermine, NMDA channel blocker, N1-dansyl-spermine, N1-DnsSpm
• Formula empirica (notazione di Hill): C₂₂H₃₇N₅O₂S · 3HCl
• Peso molecolare: 545.01
• Codice UNSPSC: 12352200
• ID PubChem: 9889212
• NACRES: NA.77

Proprietà

• Saggio: ≥97% (HPLC)
• Livello qualitativo: 100
• Forma fisica: powder
• Potenza: 0.31 μM IC₅₀
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: yellow-white
• Solubilità: DMSO: 100 mg/mL
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: CN(C)C1=CC=CC2=C1C=CC=C2S(=O)(=O)NCCCNCCCCNCCCN

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Primary Target
NMDA

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable