Flupirtine maleate

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Cat.No. 2867 - Flupirtine maleate | C15H17FN4O2.C4H4O4 | CAS No. 75507-68-5
Description: KV7 channel activator; also GABAA modulator and indirect NMDA antagonist
Alternative Names: D 9998
Chemical Name: N-[2-Amino-6-[[4-fluorophenyl)methyl]amino]-3-pyridinyl]carbamic acid ethyl ester maleate
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Reviews (2)
Literature (5)

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.

Deuterated analog also available.

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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 the degree 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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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

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


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View Related Products by Product Action

View all Voltage-gated Potassium (KV) Channel Activators

Keywords: Flupirtine maleate, 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, 2867, Tocris Bioscience

2 Citations for Flupirtine maleate

Citations are publications that use Tocris products. Selected citations for Flupirtine maleate include:

Sedivy et al (2015) Role of Kv7 channels in responses of the pulmonary circulation to hypoxia. Am J Physiol Lung Cell Mol Physiol 308 L48 PMID: 25361569

Lee et al (2014) Serum starvation-induced voltage-gated potassium channel Kv7.5 expression and its regulation by Sp1 in canine osteosarcoma cells. Int J Mol Sci 15 977 PMID: 24434641


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Reviews for Flupirtine maleate

Average Rating: 5 (Based on 2 Reviews.)

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Flupirtine maleate effect on liver injury.
By Sadequl Islam on 10/02/2018
Assay Type: In Vivo
Species: Mouse

Used flupirtine to understand how its analgesic effects correlate to its liver injury history. Flupirtine maleate dissloved easily in DMSO and worked nicely in experimental environment The product performed well under study conditions

review image

Flupirtine studied on HEK 293 cell line : Worked ideally on experiemental conditions.
By Farzana Islam on 08/24/2018
Species: Human
Cell Line/Tissue: HEK 293

The Flupirtine maleate worked excellent in study conditions and I would go back to this one everytime I need it. Flupirtine is a non-opioid non-analgesic drug prescribed in some European countries to treat post surgery patients for pain relief. My study involved investigating whether Flupirtine shows BK channel opening properties. Flupirtine works on SK channel and thus it can be speculated that it also works on BK channel to affect neuron excitability. I have used 4 different concentrations of the Flupirtine drug(0.1,1,10 and 100 microgram) to test on HEK 293 cells.NS1619 was used as a standard BK channel opener to compare its channel opening properties.

Dissolve in sterile DMSO under hood if sterile Flupirtine is required.

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Literature in this Area

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