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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.
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.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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.
Form
Yellowish-white powder
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₂₂H₃₇N₅O₂S•3HCl
Structure formula
Purity
≥97% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
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.