Molecular Weight(MW): 420.39
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.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
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4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|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.|
Flupirtine pre-incubated for 2 hours prevents cell death in rat cortical neurons induced by NMDA and gp120 of HIV-1.  Flupirtine is capable of protecting primary neurons against glutamate-induced cytotoxicity by reducing calcium ion concentrations at 1-10 mM.  Flupirtine pretreated for 2 hours preventsβ-amyloid-induced apoptosis in primary neuronal cells at concentrations of 1 or 5μg/mL.  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.  Flupirtine-maleate at concentrations of 1 μM and 10 μM decreases TRAIL-mediated death of human living brain tissue culture.  Flupirtine activates inwardly rectifying potassium ion channels and thus stabilizes the resting membrane potential at a therapeutically relevant concentration. 
|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.  Flupirtine administered centrally inhibits the nociceptive responses induced by chemical, thermal, mechanical and electrical stimuli in animal studies.  Flupirtine exerts muscle relaxant effects in rat. |
-  Perovic S, et al. Eur J Pharmacol, 1994, 288(1), 27-33.
-  Rupalla K, et al. Eur J Pharmacol, 1995, 294(2-3), 469-473
-  Müller WE, et al. J Neurochem, 1997, 68(6), 2371-237
-  Seyfried J, et al. Eur J Pharmacol, 2000, 400(2-3):155-166.
-  D?rr J, et al. J Neuroimmunol, 2005, 167(1-2), 204-209.
-  Kornhuber J, et al. J Neural Transm, 1999, 106(9-10), 857-867.
-  Block F, et al. Brain Res, 1997, 754(1-2), 279-284.
-  Bleyer H, et al. Eur J Pharmacol, 1988, 151(2), 259-265.
-  Nickel B, et al. Arzneimittelforschung, 1990, 40(8), 909-911.
|In vitro||DMSO||84 mg/mL (199.81 mM)|
|Ethanol||2 mg/mL warmed (4.75 mM)|
|In vivo||30% propylene glycol, 5% Tween 80, 65% D5W||30 mg/mL|
* 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.
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