ZK 200775

Biological Activity

ZK 200775 is a competitive AMPA/kainate antagonist. In rat cortical membranes, displays high affinity for [³H]-AMPA (K_i = 120 nM) and [³H]-CNQX (K_i = 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

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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