ZK 200775
ZK 200775 Basic information
- Product Name:
- ZK 200775
- Synonyms:
-
- [[3,4-DIHYDRO-7-(4-MORPHOLINYL)-2,3-DIOXO-6-(TRIFLUOROMETHYL)-1(2H)-QUINOXALINYL]METHYL]PHOSPHONIC ACID
- ZK 200775
- [[3,4-Dihydro-7-(4-morpholinyl)-2,3-dioxo-6-(trifluoromethyl)-1(2H)-quinoxalinyl]methyl]phosphonicacid
- Fanapanel
- MPQX
- 7-Morpholino-2,3-dioxo-6-(trifluoromethyl)-1,2,3,4-tetrahydroquinoxalin-1-ylmethylphosphonic acid
- [[3,4-Dihydro-7-(4-morpholinyl)-2,3-dioxo-6-(trifluoromethyl)-1(2H)-quinoxalinyl]methyl]-phosphonic acid hydrate
- P-[[3,4-Dihydro-7-(4-morpholinyl)-2,3-dioxo-6-(trifluoromethyl)-1(2H)-quinoxalinyl]methyl]phosphonic acid
- CAS:
- 161605-73-8
- MF:
- C14H15F3N3O6P
- MW:
- 409.25
- Mol File:
- 161605-73-8.mol
ZK 200775 Chemical Properties
- Density
- 1.615±0.06 g/cm3(Predicted)
- storage temp.
- Inert atmosphere,2-8°C
- solubility
- DMSO: ≥20mg/mL
- pka
- 2.09±0.10(Predicted)
- form
- powder
- color
- off-white to light brown
ZK 200775 Usage And Synthesis
Uses
ZK 200775 is a competitive AMPA/kainate antagonist. Neuronal protection against cerebral ischemia.
Biological Activity
Competitive AMPA/kainate antagonist. In rat cortical membranes, displays high affinity for [ 3 H]-AMPA (K i = 120 nM) and [ 3 H]-CNQX (K i = 32 nM) binding sites and low affinity for kainate and NMDA channel-associated binding sites (IC 50 values range from 2.5 to 11 μ M). Inhibits currents induced by AMPA, kainate and NMDA with IC 50 values of 21 nM, 27 nM, and > 1 μ M respectively. Displays anxiolytic, anticonvulsant and muscle relaxant activity in vivo .
in vivo
ZK200775 elevated the threshold for AMPA- and kainate-induced clonic seizures in mice with a THRD50 (threshold dose) of 2.9 (1.7–4.6) and 1.6 (1.3–2.0) mg/kg i.v., whereas the threshold for NMDA-induced seizures was elevated only in doses, THRD50 of 24.1 (21.9–26.5) mg/kg i.v., which affected motor coordination in the rotating rod, ED50 14.6 (12.1–17.6) mg/kg. ZK200775 in doses of 10 and 30 mg/kg i.v. reduced muscle tone in genetically spastic rats [1]. ZK200775 (3.0 but not 1.5 or 6.0 mg/kg) significantly decreased the nicotine-induced (0.6 mg/kg) DA release in the NAcc and nicotine-stimulated LMA. ZK200775 (1.5, 3.0, 6.0 mg/kg) alone influenced neither DA release nor LMA. ZK200775 showed 34-fold selectivity for AMPA receptors compared to NMDA receptors and no affinity to nicotine receptors
storage
Desiccate at +4°C
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