For research use only.
CAS No. 75507-68-5
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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|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. |
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-  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||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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