AMG-9810 is a potent, selective and competitive TRPV1 antagonist with IC50 of 24.5 and 85.6 nM for human and rat TRPV1, respectively.
AMG-9810 blocks capsaicin-evoked depolarization and CGRP release in cultures of rat dorsal root ganglion primary neurons.
AMG-9810 is the first cinnamide TRPV1 antagonist reported to block capsaicin-induced eye wiping behavior and reverse hyperalgesia in an animal model of inflammatory pain.
