5.05764
NMDA Antagonist XI, N1-dansyl-spermine
别名:
NMDA Antagonist XI, N1-dansyl-spermine, NMDA channel blocker, N1-dansyl-spermine, N1-DnsSpm
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关于此项目
经验公式（希尔记法）:
C22H37N5O2S · 3HCl
分子量:
545.01
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
PubChem Substance ID:
InChI
1S/C22H37N5O2S/c1-27(2)21-11-5-10-20-19(21)9-6-12-22(20)30(28,29)26-18-8-17-25-15-4-3-14-24-16-7-13-23/h5-6,9-12,24-26H,3-4,7-8,13-18,23H2,1-2H3
InChI key
NSUSGNAFCIMCDH-UHFFFAOYSA-N
SMILES string
CN(C)C1=CC=CC2=C1C=CC=C2S(=O)(=O)NCCCNCCCCNCCCN
assay
≥97% (HPLC)
form
powder
potency
0.31 μM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow-white
solubility
DMSO: 100 mg/mL
Quality Level
General description
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 Actions
Primary Target
NMDA
NMDA
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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