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AMG 517 is an antagonist of transient receptor potential vanilloid 1 (TRPV1; IC50 = 0.9 nM).1 It inhibits mechanical and thermal allodynia in a rat model of burn injury when administered intrathecally at a dose of 165 µg.2 AMG 517 (150 and 300 µg/kg) also reverses increases in the level of calcitonin gene-related peptide (CGRP) and increases expression of GFAP and GAP-43 in the dorsal horn of the spinal cord, as well as enhances axonal regeneration in a rat model of sciatic nerve transection injury.3
WARNING This product is not for human or veterinary use.
1. Discovery of novel 6,6-
2. Central activation of TRPV1 and TRPA1 by novel endogenous agonists contributes to mechanical allodynia and thermal hyperalgesia after burn injury. Mol. Pain 12, (2016).
3. Attenuation of TRPV1 by AMG-