product name Flupirtine maleate
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.
References: Eur J Pharmacol. 1994 Dec 15;288(1):27-33; Eur J Pharmacol. 1995 Dec 29;294(2-3):469-73.
420.39
Formula
C15H17FN4O2·C4H4O4
CAS No.
75507-68-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 84 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL (4.8 mM)
Solubility (In vivo)
30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19413590
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: 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. |
|---|---|
| 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. |
| Animal model | Male Wistar rats with cerebral ischemia induced by four-vessel-occlusion |
| Formulation & Dosage | Formulated in 0.9% sodium chloride solution; 5 mg/kg; i.p. injection |
| References | Eur J Pharmacol. 1994 Dec 15;288(1):27-33; Eur J Pharmacol. 1995 Dec 29;294(2-3):469-73; Brain Res. 1997 Apr 18;754(1-2):279-84. |
