| Bioactivity | Flupirtine Maleate is a brain penetrant, and orally bioavailable, non-opioid and centrally acting analgesic agent. Flupirtine Maleate is an indirect N-methyl-D-aspartate receptor (NMDAR) antagonist. Neuroprotective properties[1][2]. |
| Invitro | Flupirtine (0.1, 1, and 10 mM; 24 hours) significantly reduces the growth and viability of U373 malignant glioma cells with the GI50 of 0.47 mM. Flupirtine has neuroprotective effect of on U373 MG cells[3].Flupirtine Maleate is active at the KCNQ and GABAA channels in the range of 10-30 μM[4] Cell Viability Assay[3] Cell Line: |
| In Vivo | Flupirtine (5 and 10 mg/kg) induces acute neuroprotection, reduces motor coordination impairment and ameliorates recombinant tissue plasminogen activator (rtPA)-induced toxicity[2]. Animal Model: |
| Name | Flupirtine Maleate |
| CAS | 75507-68-5 |
| Formula | C19H21FN4O6 |
| Molar Mass | 420.39 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Jan Dörr,et al. Disease Modification in Multiple Sclerosis by Flupirtine-Results of a Randomized Placebo Controlled Phase II Trial. Front Neurol. 2018 Oct 9;9:842. [2]. Hanna M Jaeger, et al. The indirect NMDAR inhibitor flupirtine induces sustained post-ischemic recovery, neuroprotection and angioneurogenesis. Oncotarget. 2015 Jun 10;6(16):14033-44. [3]. Elango Panchanathan,Effect of flupirtine on the growth and viability of U373 malignant glioma cells.Cancer Biol Med. 2013 Sep;10(3):142-7. [4]. Martin J Gunthorpe,et al. The mechanism of action of retigabine (ezogabine), a first-in-class K+ channel opener for the treatment of epilepsy.Epilepsia. 2012 Mar;53(3):412-24. |