QX-314 bromide is a membrane-impermeable permanently charged sodium channel blocker^[1]. IC50 & Target: sodium channel^[1] In Vitro: QX-314 bromide exerts biphasic effects on transient receptor potential vanilloid subtype 1 channels (TRPV1) in vitro ^[1].
QX-314 bromide (1–60 mM) directly activates TRPV1 in a concentration-dependent manner^[1].
QX-314 bromide (≥ 30 mM) produces oocyte membrane blackening and cell death ^[1].
QX-314 bromide inhibits calcium currents in hippocampal CA1 pyramidal neurons intracellular, and the low-threshold (T-type) Ca²⁺ currents are on average < 10% of control amplitude ^[3].
QX-314 bromide shifts the current-voltage relationships (I-Vs) in the positive voltage direction due to the presence of intracellular Br- ^[3].
In Vivo: QX-314 bromide (1.6 mg/kg; i.c.) abolishes responses to noxious mechanical and thermal stimuli without motor or tactile deficits when co-treatment with capsaicin^[2].