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Submit ReviewFlupirtine maleate is a 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.
Flupirtine maleate is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 420.4 |
公式 | C15H17FN4O2.C4H4O4 |
储存 | Desiccate at +4°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 42.04 | 100 | |
ethanol | 4.2 | 10 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for Flupirtine maleate, please let us know.
关键词: 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
引用文献是使用了 Tocris 产品的出版物。 Flupirtine maleate 的部分引用包括:
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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平均评分: 5 (基于 2 条评论。)
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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
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.