Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Elect...
Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release
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Author / Creator
Alexandrou, Aristos J , Brown, Adam R , Chapman, Mark L , Estacion, Mark , Turner, Jamie , Mis, Malgorzata A , Wilbrey, Anna , Payne, Elizabeth C , Gutteridge, Alex , Cox, Peter J , Doyle, Rachel , Printzenhoff, David , Lin, Zhixin , Marron, Brian E , West, Christopher , Swain, Nigel A , Storer, R Ian , Stupple, Paul A , Castle, Neil A , Hounshell, James A , Rivara, Mirko , Randall, Andrew , Dib-Hajj, Sulayman D , Krafte, Douglas , Waxman, Stephen G , Patel, Manoj K , Butt, Richard P and Stevens, Edward B
Publisher
United States: Public Library of Science
Journal title
Language
English
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Publisher
United States: Public Library of Science
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Contents
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-0508977...
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Full title
Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release
Authors, Artists and Contributors
Author / Creator
Brown, Adam R
Chapman, Mark L
Estacion, Mark
Turner, Jamie
Mis, Malgorzata A
Wilbrey, Anna
Payne, Elizabeth C
Gutteridge, Alex
Cox, Peter J
Doyle, Rachel
Printzenhoff, David
Lin, Zhixin
Marron, Brian E
West, Christopher
Swain, Nigel A
Storer, R Ian
Stupple, Paul A
Castle, Neil A
Hounshell, James A
Rivara, Mirko
Randall, Andrew
Dib-Hajj, Sulayman D
Krafte, Douglas
Waxman, Stephen G
Patel, Manoj K
Butt, Richard P
Stevens, Edward B
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Primary Identifiers
Record Identifier
TN_cdi_plos_journals_1779034067
Permalink
https://devfeature-collection.sl.nsw.gov.au/record/TN_cdi_plos_journals_1779034067
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ISSN
1932-6203
E-ISSN
1932-6203
DOI
10.1371/journal.pone.0152405