Quaternary Lidocaine Derivative QX-314 Activates and Permeates Human TRPV1 and TRPA1 to Produce Inhibition of Sodium Channels and Cytotoxicity.

@article{Stueber2016QuaternaryLD,
  title={Quaternary Lidocaine Derivative QX-314 Activates and Permeates Human TRPV1 and TRPA1 to Produce Inhibition of Sodium Channels and Cytotoxicity.},
  author={Thomas J. Stueber and Mirjam J. Eberhardt and Christoph Hadamitzky and Annette Jangra and Stefan Schenk and Felicia Dick and Carsten Stoetzer and Katrin Kistner and Peter W Reeh and Alexander M. Binshtok and Andreas Leffler},
  journal={Anesthesiology},
  year={2016},
  volume={124 5},
  pages={1153-65}
}
BACKGROUND The relatively membrane-impermeable lidocaine derivative QX-314 has been reported to permeate the ion channels transient receptor potential vanilloid 1 (TRPV1) and transient receptor potential cation channel, subfamily A, member 1 (TRPA1) to induce a selective inhibition of sensory neurons. This approach is effective in rodents, but it also seems to be associated with neurotoxicity. The authors examined whether the human isoforms of TRPV1 and TRPA1 allow intracellular entry of QX-314… CONTINUE READING