Patent ID: 8486647

Claim:
A method for identifying a Na v 1.7 antagonist, comprising: (a) providing ex vivo a cell that expresses a full-length human Na v 1.7 α subunit protein, or a chimeric Na v 1.7 α subunit protein comprising an extracellular loop of domain I or Ill of the mouse Na v 1.7 α subunit that has been replaced by the corresponding loop from a human Na v 1.7 α subunit; (b) contacting the cell with a test compound that binds to, or blocks a function of, the human Na v 1.7 α subunit protein or the chimeric Na v 1.7 α subunit protein of (a) and waiting a first period of time; (c) contacting the cell from (b) with one or more inflammatory substances and waiting a second period of time; (d) determining the amount of calcitonin gene-related peptide (CGRP) released from the cell following step (c); and (e) comparing the amount of CGRP released in step (d) to the amount of CGRP released in the presence of a known sodium channel inhibitor, wherein an increase in CGRP released in the presence of a test compound indicates inhibition of Na v 1.7.