Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release

@inproceedings{Alexandrou2016SubtypeSelectiveSM,
  title={Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release},
  author={Aristos J. Alexandrou and Adam R. Brown and Mark L. Chapman and Mark Estacion and Jamie K. Turner and Malgorzata A Mis and Anna Wilbrey and Elizabeth C. Payne and Alex Gutteridge and Peter J. Cox and Rachel Doyle and David M Printzenhoff and Zhixin Lin and Brian E. Marron and Christopher L West and Nigel A Swain and R. Ian Storer and Paul A. Stupple and Neil A Castle and James A. Hounshell and Mirko Rivara and Andrew Randall and Sulayman D. Dib-Hajj and Douglas S. Krafte and Stephen G. Waxman and Manoj K Patel and Richard Butt and Edward B. Stevens},
  booktitle={PloS one},
  year={2016}
}
Human genetic studies show that the voltage gated sodium channel 1.7 (Nav1.7) is a key molecular determinant of pain sensation. However, defining the Nav1.7 contribution to nociceptive signalling has been hampered by a lack of selective inhibitors. Here we report two potent and selective arylsulfonamide Nav1.7 inhibitors; PF-05198007 and PF-05089771, which we have used to directly interrogate Nav1.7's role in nociceptor physiology. We report that Nav1.7 is the predominant functional TTX… CONTINUE READING
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