Flupirtine

Flupirtine (0.1-100 μM for tsA cells; 3-30 μM for SCG neurons; 3-30 μM for hippocampal, DRG, DH neurons) enhances currents through K_V7 channels in tsA 201 cells expressing K_V7.2/7.3 subunits, rat SCG neurons, hippocampal neurons, DRG neurons, and DH neurons with EC₅₀ values ranging from 4.4 to 6.1 μM^[2].
Flupirtine (10, 30 μM) modulates GABA_A receptors (enhancing low-concentration GABA currents) and NMDA receptors (inhibiting at 30 μM) but not TRPV1, non-NMDA glutamate, or glycine receptors in rat hippocampal neurons^[2].
Flupirtine (30 μM) potentiates GABA_A receptors in rat DRG, DH, and SCG neurons, with greater leftward shifts of GABA concentration-response curves in DRG and DH neurons than SCG neurons^[2].
Flupirtine (0.1-100 μM) is more potent at enhancing GABA_A receptor currents in rat DRG neurons (EC₅₀ 22 μM) than DH (EC₅₀ 53 μM) or hippocampal (EC₅₀ 65 μM) neurons, and therapeutic concentrations (3 μM) facilitate K_V7 channels and GABA_A receptors similarly in DRG/DH neurons^[2].
Flupirtine (10-300 μM; 1.5 minutes) antagonizes NMDA-induced currents in cultured rat superior colliculus neurones with an IC₅₀ of 182.1 μM for steady-state responses and 228.6 μM for peak responses^[3].
Flupirtine (0.001-10 mM; 24 h) inhibits the growth of U373 MG cells with a GI₅₀ of 0.47 mM, showing significant growth reduction at 1 and 10 mM after 24 h^[4].
Flupirtine (1 mM; 24, 48 h) alters the cell cycle distribution of U373 MG cells, decreasing the percentage of cells in the G₀-G₁ phase compared to control after 24 and 48 h, with significant variations in cell cycle phases observed after 48 h^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.