ZK 200775 CAS: 161605-73-8
MF: C14H15N3O6F3P
MW: 409.25
A competitive AMPA/kainate antagonist.

ZK 200775 (CAS 161605-73-8)

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Synonym: MPQX
Application: A competitive AMPA/kainate antagonist
CAS Number: 161605-73-8
Molecular Weight: 409.25
Molecular Formula: C14H15N3O6F3P
* Refer to Certificate of Analysis for lot specific data (including water content).
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ZK 200775 is a competitive GluR (AMPA)/kainate antagonist. In rat cortical membranes, it displays high affinity for [3H]-AMPA (Ki = 120 nM) and [3H]-CNQX (Ki = 32 nM) binding sites but low affinity for kainate and NMDA channel-associated binding sites (IC50 values range from 2.5 to 11 μM). It inhibits currents induced by AMPA, kainate and NMDA with IC50 values of 21 nM, 27 nM, and > 1 μM respectively. AMPA is a transmembrane glutamate receptor composed of the subunits GluR-1,2,3,4.


References

Turski et al (1998) ZK200775: a phosphonate quinoxalinedione AMPA antagonist for neuroprotection in stroke and trauma. 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 CGP39551. Pychopharmacology 175 114. Elger et al (2005) Novel a-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.

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and ethanol (50 mM).
Storage :
Desiccate at 4° C
Melting Point :
90.27° C (Predicted)
Boiling Point :
480.00° C (Predicted)
Density :
1.62 g/cm3 (Predicted)
Refractive Index :
n20D 1.56 (Predicted)
IC50 :
currents induced by AMPA: IC50 = 21 nM; currents induced by kainate: IC50 = 27 nM; Xenopus sp.: IC50 = 31 nM; Glutamate receptor ionotropic, AMPA: IC50 = 140 nM (rat); currents induced by NMDA: IC50 = > 1 µM
Ki Data :
[3H]-CNQX: Ki= 32 nM (rat cortical membranes); [3H]-AMPA : Ki= 120 nM (rat cortical membranes); DCKA binding site: Ki= 2.8 µM
pK Values :
pKa: 1.44 (Predicted), pKb: 2.8 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
RTECS :
SZ7655100
PubChem CID :
208953
MDL Number :
MFCD07364000
SMILES :
C1COCCN1C2=CC3=C(C=C2C(F)(F)F)NC(=O)C(=O)N3CP(=O)(O)O

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Certificate of Analysis

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