5.05764

NMDA Antagonist XI, N1-dansyl-spermine

• Synonym(e): NMDA Antagonist XI, N1-dansyl-spermine, NMDA channel blocker, N1-dansyl-spermine, N1-DnsSpm
• Empirische Formel (Hill-System): C₂₂H₃₇N₅O₂S · 3HCl
• Molekulargewicht: 545.01
• UNSPSC-Code: 12352200
• PubChem Substanz-ID: 9889212
• NACRES: NA.77

Eigenschaften

• Assay: ≥97% (HPLC)
• Qualitätsniveau: 100
• Form: powder
• Wirksamkeit: 0.31 μM IC₅₀
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: yellow-white
• Löslichkeit: DMSO: 100 mg/mL
• Lagertemp.: 2-8°C
• SMILES String: CN(C)C1=CC=CC2=C1C=CC=C2S(=O)(=O)NCCCNCCCCNCCCN

Beschreibung

Allgemeine Beschreibung

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.

Biochem./physiol. Wirkung

Primary Target
NMDA

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable