Biological Activity
Non-opioid analgesic with muscle relaxant properties. Activates KV7 potassium channels, indirectly antagonizes NMDA receptors and modulates GABAA receptors. Exhibits neuroprotective actions in a model of cerebral ischemia in mice and reduces apoptosis and necrosis induced by noxious stimuli.
Compound Libraries
Flupirtine maleate is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 420.4 |
| Formula | C15H17FN4O2.C4H4O4 |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 75507-68-5 |
| PubChem ID | 53276 |
| InChI Key | JUUFBMODXQKSTD-UHFFFAOYSA-N |
| Smiles | OC(=O)C=C/C(O)=O.NC1=C(NC(OCC)=O)C=CC(NCC2=CC=C(F)C=C2)=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.04 | 100 | |
| ethanol | 4.2 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 420.4. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.38 mL | 11.89 mL | 23.79 mL |
| 5 mM | 0.48 mL | 2.38 mL | 4.76 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.38 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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References
References are publications that support the products' biological activity.
Osborne et al (1998) Flupirtine, a nonopioid centrally acting analgesic, acts as an NMDA antagonist. Gen.Pharmacol. 30 255 PMID: 9510072
Azad et al (2004) The potassium channel modulator flupirtine shifts the frequency-response function of hippocampal synapses to favour LTD in mice. Neurosci.Lett. 370 186 PMID: 15488320
Yeung et al (2007) Molecular expression and pharmacological identification of a role for Kv7 channels in murine vascular reactivity. Br.J.Pharmacol. 151 758 PMID: 17519950
Klinger (2012) Concomitant facilitation of GABAA receptors and KV7 channels by the non-opioid analgesic flupirtine. Br.J.Pharmacol. 166 1631 PMID: 22188423
Keywords: Flupirtine maleate, supplier, K+, channel, activators, Indirect, NMDA, receptors, antagonists, Potassium, Channels, kv7, GABA, GABAA, Glutamate, Receptors, N-Methyl-D-Aspartate, iGluR, Ionotropic, D9998, D, 9998, Voltage-Gated, Potassium, Channels, NMDA, Receptors, GABAA, Receptors, Voltage-Gated, Potassium, Channels, Tocris Bioscience
