ZK 200775

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ZK 200775 | CAS No. 161605-73-8 | AMPA Receptor Antagonists
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Description: Competitive non-NMDA iGluR antagonist
Alternative Names: MPQX

Chemical Name: [[3,4-Dihydro-7-(4-morpholinyl)-2,3-dioxo-6-(trifluoromethyl)-1(2H)-quinoxalinyl]methyl]phosphonic acid

Purity: ≥99%

Product Details
Citations (1)
Reviews

Biological Activity

Competitive AMPA/kainate antagonist. In rat cortical membranes, displays high affinity for [3H]-AMPA (Ki = 120 nM) and [3H]-CNQX (Ki = 32 nM) binding sites and low affinity for kainate and NMDA channel-associated binding sites (IC50 values range from 2.5 to 11 μM). Inhibits currents induced by AMPA, kainate and NMDA with IC50 values of 21 nM, 27 nM, and > 1 μM respectively. Displays anxiolytic, anticonvulsant and muscle relaxant activity in vivo.

Technical Data

M.Wt:
409.25
Formula:
C14H15N3O6F3P
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in ethanol
Purity:
≥99%
Storage:
Desiccate at +4°C
CAS No:
161605-73-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. X-ray structure, symmetry and mechanism of an AMPA-subtype glutamate receptor.
    Sobolevsky
    Nature, 2009;462:745
  2. Novel α-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptor antagonists of 2,3-benzodiazepine type: chemical synthesis, in vitro characterization, and in vivo prevention of acute neurodegeneration.
    Elger et al.
    J.Med.Chem., 2005;48:4618
  3. ZK200775: a phosphonate quinoxalinedione AMPA antagonist for neuroprotection in stroke and trauman
    Turski et al.
    Proc.Natl.Acad.Sci.USA., 1998;95:10960
  4. Nicotine-induced DA release in the nucleus accumbens is inhibited by the novel AMPA antagonist ZK200775 and the NMDA antagonist CGP39551n
    Kosowski et al.
    Pychopharmacology, 2004;175:114

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Citation for ZK 200775

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