5.04535
QNZ46
别名:
QNZ46, NMDA Antagonist VIII, 4-[6-Methoxy-2-[(1E)-2-(3-nitrophenyl)ethenyl]-4-oxo-3(4H)-quinazolinyl]-Benzoic acid
InChI
1S/C24H17N3O6/c1-33-19-10-11-21-20(14-19)23(28)26(17-8-6-16(7-9-17)24(29)30)22(25-21)12-5-15-3-2-4-18(13-15)27(31)32/h2-14H,1H3,(H,29,30)/b12-5+
InChI key
GNLVJIICVWDSNI-LFYBBSHMSA-N
assay
≥98% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 5 mg/mL
Quality Level
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General description
A noncompetitive and voltage-independent antagonist selective for NR2C/D containing NMDA receptors (IC50 = 6, 3, 229, and >300 µM for NR2C, NR2D, NR2A, and NR2B, respectively). Inhibition on NR2C/D containing NMDA receptors is glutamate-binding, but not glycine-binding, dependent. Represents a new class of noncompetitive subunit-selective NMDA receptor antagonists. With more than 100-fold selectivity for recombinant NMDA receptors over AMPA and kainate receptors.
Biochem/physiol Actions
Primary Target
NMDA receptors
NMDA receptors
Target IC50: 6, 3, 229, and >300 →M for NR2C, NR2D, NR2A, and NR2B, respectively.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Slight warming is required for complete solubilization.
Other Notes
Mayer, M., et al. 2013. Annu. Rev. Physiol.75, 1.
Hansen, K., 2011. J. Neurosci.9, 3650.
Mosley, C., et al. 2010. J. Med. Chem.53, 5476.
Hansen, K., 2011. J. Neurosci.9, 3650.
Mosley, C., et al. 2010. J. Med. Chem.53, 5476.
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
法规信息
新产品
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Kasper B Hansen et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 31(10), 3650-3661 (2011-03-11)
NMDA receptors are ionotropic glutamate receptors that mediate excitatory synaptic transmission and have been implicated in several neurological diseases. We have evaluated the mechanism of action of a class of novel subunit-selective NMDA receptor antagonists, typified by (E)-4-(6-methoxy-2-(3-nitrostyryl)-4-oxoquinazolin-3(4H)-yl)-benzoic acid (QNZ46).
Cara A Mosley et al.
Journal of medicinal chemistry, 53(15), 5476-5490 (2010-08-06)
We describe a new class of subunit-selective antagonists of N-methyl D-aspartate (NMDA)-selective ionotropic glutamate receptors that contain the (E)-3-phenyl-2-styrylquinazolin-4(3H)-one backbone. The inhibition of recombinant NMDA receptor function induced by these quinazolin-4-one derivatives is noncompetitive and voltage-independent, suggesting that this family
Janesh Kumar et al.
Annual review of physiology, 75, 313-337 (2012-09-15)
X-ray crystal structures for the soluble amino-terminal and ligand-binding domains of glutamate receptor ion channels, combined with a 3.6-Å-resolution structure of the full-length AMPA receptor GluA2 homotetramer, provide unique insights into the mechanisms of the assembly and function of glutamate
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