| Bioactivity | QX-314 bromide is a membrane-impermeable permanently charged sodium channel blocker[1]. |
| Target | sodium channel |
| Invitro | 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]. Animal Model: |
| Name | QX-314 bromide |
| CAS | 24003-58-5 |
| Formula | C16H27BrN2O |
| Molar Mass | 343.30 |
| 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]. Rivera-Acevedo RE, et al. The quaternary lidocaine derivative, QX-314, exerts biphasic effects on transient receptor potential vanilloid subtype 1 channels in vitro. Anesthesiology. 2011 Jun;114(6):1425-34. [2]. Binshtok AM, et al. Coapplication of lidocaine and the permanently charged sodium channel blocker QX-314 produces a long-lasting nociceptive blockade in rodents. Anesthesiology. 2009 Jul;111(1):127-37. [3]. Talbot MJ, et al. Intracellular QX-314 inhibits calcium currents in hippocampal CA1 pyramidal neurons. J Neurophysiol. 1996 Sep;76(3):2120-4. |