[CAS NO. 161605-73-8] Fanapanel
PRODUCTS SPECIFICATIONS [161605-73-8]
DESCRIPTION [161605-73-8]
Overview
| MDL | MFCD07364000 |
|---|---|
| Molecular Weight | 409.25 |
| Molecular Formula | C14H15F3N3O6P |
| SMILES | O=C(N1CP(O)(O)=O)C(NC(C1=C2)=CC(C(F)(F)F)=C2N3CCOCC3)=O |
Summary
Fanapanel (ZK200775) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.
IC50 & Target
|
AMPA Receptor |
In Vitro
In the cortical slice preparation assay, ZK200775 gave Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively. In the spreading depression assay, it gave IC50 values of 200 nM, 76 nM, 13 μM, and 18 μM against quisqualate, kainate, NMDA, and glycine [1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00999284 | Charite University, Berlin, Germany|Bayer |
Visual Acuity
|
December 1996 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 1.25 mg/mL ( 3.05 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4435 mL | 12.2175 mL | 24.4349 mL |
| 5 mM | --- | --- | --- |
| 10 mM | --- | --- | --- |
References
- [1] Turski L, et al. ZK200775: a phosphonate quinoxalinedione AMPA antagonist for neuroprotection in stroke and trauma. Proc Natl Acad Sci U S A. 1998 Sep 1;95(18):10960-5.
- [2] Kosowski AR, et al. Nicotine-induced dopamine release in the nucleus accumbens is inhibited by the novel AMPA antagonist ZK200775 and the NMDA antagonist CGP39551. Psychopharmacology (Berl). 2004 Aug;175(1):114-23.
Synonyms
