Cat. No. 2345
Alternative Name: MPQX
Chemical Name: [[3,4-Dihydro-7-(4-morpholinyl)-2,3-dioxo-6-(trifluoromethyl)-1(2H)-quinoxalinyl]methyl]phosphonic acid
Biological ActivityCompetitive 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
Turski et al (1998) ZK200775: a phosphonate quinoxalinedione AMPA antagonist for neuroprotection in stroke and trauman Proc.Natl.Acad.Sci.USA. 95 10960.
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.
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.
Sobolevsky (2009) X-ray structure, symmetry and mechanism of an AMPA-subtype glutamate receptor. Nature 462 745. PMID: 19946266.
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Keywords: ZK 200775, supplier, Competitive, AMPA/kainate, antagonists, Glutamate, Receptors, iGluR, Ionotropic, ZK200775
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