Flupirtine maleate

Catalog No.S1334 Batch:S133401

Technical Data

Formula	C₁₅H₁₇FN₄O₂·C₄H₄O₄
Molecular Weight	420.39	CAS No.	75507-68-5
Solubility (25°C)*	In vitro	DMSO	84 mg/mL (199.81 mM)
		Ethanol	3 mg/mL (7.13 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Flupirtine maleate is the salt form of Flupirtine, which is a centrally acting non-opioid analgesia, is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties.

Targets

NMDA receptor ^[1]

Potassium channel ^[6]

In vitro

Flupirtine pre-incubated for 2 hours prevents cell death in rat cortical neurons induced by NMDA and gp120 of HIV-1. ^[1] Flupirtine is capable of protecting primary neurons against glutamate-induced cytotoxicity by reducing calcium ion concentrations at 1-10 mM. ^[2] Flupirtine pretreated for 2 hours preventsβ-amyloid-induced apoptosis in primary neuronal cells at concentrations of 1 or 5μg/mL. ^[3] Flupirtine at concentration of 10 μM markedly decreases nonreceptor-mediated necrotic cell death in PC 12 cultures treated with 10 mM L-glutamate, meanwhile, Flupirtine exerts anti-oxidative effects in PC 12 cultures. ^[4] Flupirtine-maleate at concentrations of 1 μM and 10 μM decreases TRAIL-mediated death of human living brain tissue culture. ^[5] Flupirtine activates inwardly rectifying potassium ion channels and thus stabilizes the resting membrane potential at a therapeutically relevant concentration. ^[6]

In vivo

Pre-treatment with Flupirtine exerts a protective effect on hippocampal and striatal neuronal damage and on deficits in spatial learning in rats with cerebral ischemia. ^[7] Flupirtine administered centrally inhibits the nociceptive responses induced by chemical, thermal, mechanical and electrical stimuli in animal studies. ^[8] Flupirtine exerts muscle relaxant effects in rat. ^[9]

Protocol (from reference)

Cell Assay:^{^[4]}	Cell lines PC12 cell Concentrations 1 or 5 μg/mL Incubation Time 72 hours Method For measurement of viability and generation of reactive oxygen intermediates, PC12 cells are seeded in 24- or 96-well plates coated with poly-L-lysine at 10⁵ cells/mL. Drugs are dissolved in PBS (pH 7.4), or ethanol and filtered sterile. At the end of each experiment cells are trypsinized and pelleted together with cells of the culture supernatant. After staining for 10 min with 0.2% Trypan blue solution live (unstained) and dead (Trypan blue positive) cells are counted in a hemocytometer chamber. In addition, cellular viability is evaluated by the reduction of MTT to formazan. After 2 hours incubation with MTT (0.5 mg/ml) at 37 °C, cells are lysed in DMSO. Extinction at 570 nm is determined on a plate photometer. For staining of surviving adherent cells, plates are incubated for 10 min with 0.5% crystalviolet dissolved in 20% methanol. Plates are rinsed with water and stained cells are lysed in 50% ethanol, 0.1 M sodiumcitrate before determining extinction at 550 nm.
Animal Study:^{^[7]}	Animal Models male Wistar rats with cerebral ischemia induced by four-vessel-occlusion Dosages 5 mg/kg Administration Intraperitoneal injection either 20 min before and 50 min after occlusion or directly and 70 min after occlusion

Cell Assay:^{^[4]}

Cell lines
PC12 cell
Concentrations
1 or 5 μg/mL
Incubation Time
72 hours
Method
For measurement of viability and generation of reactive oxygen intermediates, PC12 cells are seeded in 24- or 96-well plates coated with poly-L-lysine at 10⁵ cells/mL. Drugs are dissolved in PBS (pH 7.4), or ethanol and filtered sterile. At the end of each experiment cells are trypsinized and pelleted together with cells of the culture supernatant. After staining for 10 min with 0.2% Trypan blue solution live (unstained) and dead (Trypan blue positive) cells are counted in a hemocytometer chamber. In addition, cellular viability is evaluated by the reduction of MTT to formazan. After 2 hours incubation with MTT (0.5 mg/ml) at 37 °C, cells are lysed in DMSO. Extinction at 570 nm is determined on a plate photometer. For staining of surviving adherent cells, plates are incubated for 10 min with 0.5% crystalviolet dissolved in 20% methanol. Plates are rinsed with water and stained cells are lysed in 50% ethanol, 0.1 M sodiumcitrate before determining extinction at 550 nm.

Animal Study:^{^[7]}

Animal Models
male Wistar rats with cerebral ischemia induced by four-vessel-occlusion
Dosages
5 mg/kg
Administration
Intraperitoneal injection either 20 min before and 50 min after occlusion or directly and 70 min after occlusion

References

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Selleck's Flupirtine maleate has been cited by 2 publications

Development of an Electrophysiological Assay for Kv7 Modulators on IonWorks Barracuda. [ Assay Drug Dev Technol, 2019, 17(7):310-321]	PubMed: 31634018
Noise-induced plasticity of KCNQ2/3 and HCN channels underlies vulnerability and resilience to tinnitus [ Elife, 2015, 4]	PubMed: 26312501

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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