ZK 200775

Cat. No. 2345

ZK 200775 C14H15N3O6F3P [161605-73-8]

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Alternative Name: MPQX

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

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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

Sobolevsky (2009) X-ray structure, symmetry and mechanism of an AMPA-subtype glutamate receptor. Nature 462 745. PMID: 19946266.

Elger et al (2005) 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. J.Med.Chem. 48 4618. PMID: 15999999.

Kosowski et al (2004) Nicotine-induced dopamine release in the nucleus accumbens is inhibited by the novel AMPA antagonist ZK200775 and the NMDA antagonist CGP39551n Pychopharmacology 175 114.

Turski et al (1998) ZK200775: a phosphonate quinoxalinedione AMPA antagonist for neuroprotection in stroke and trauman Proc.Natl.Acad.Sci.USA. 95 10960.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for ZK 200775 include:

Lesne et al (2005) Akt-dependent expression of NAIP-1 protects neurons against amyloid-{beta} toxicity. J Biol Chem 280 24941. PMID: 15797869.

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Keywords: ZK 200775, supplier, Competitive, AMPA/kainate, antagonists, Glutamate, Receptors, iGluR, Ionotropic, ZK200775, Tocris Bioscience, AMPA Receptor Antagonist products

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