AMG-517

AMG-517 is an antagonist of transient receptor potential vanilloid 1 (TRPV1) with an IC₅₀ of 0.9 nM. It inhibits post-burn mechanical and thermal allodynia in a rat model of burn injury when administered intrathecally at a dose of 165 µg. It (150 and 300 µg/kg) decreases calcitonin gene-related peptide (CGRP) release from spinal dorsal horn and promotes peripheral nerve regeneration in a rat model of sciatic nerve transection injury.