化学性质：                                                                                                             

产品描述：                                                                                                            

QX-314 is a positively charged, membrane-impermeable quaternary lidocaine derivative [1][2][3][4].

QX-314 is a local anesthetic. In CAl pyramidal neurons of the guinea-pig hippocampal slice, QX-314 blocked both Na+ dependent action potentials and the voltage-dependent, non-inactivating Na+ conductance [1]. In Xenopus laevis oocytes expressed TRPV1 and TRPV4 channels, QX-314 (10, 30, and 60 mM) activated TRPV1 channels, but not TRPV4 channels. QX-314 at lower concentrations (less than 1mM) potently inhibited capsaicin-evoked TRPV1 currents with IC50 value of 8.0 μM. In TRPV1-expressing tsA201 cells, QX-314 induced transient increase in cytoplasmic Ca2+ [2].  In large-diameter human DRG neurons, flagellin/QX-314 inhibited sodium currents [3].

In three standard local anesthetic animal models, QX-314 reversibly and concentration-dependently induced long-lasting local anesthesia with a slow onset [4]. Intraplantar co-application of flagellin/QX-314 inhibited mechanical allodynia after nerve injury, chemotherapy and diabetic neuropathy in a dose-dependent way. In naive and chemotherapy-treated mice, co-application of flagellin/QX-314 selectively inhibited Aβ-fiber conduction [3].

特别提醒：