Description
A-967079 (1170613-55-4) is a TRPA1 blocker. Active in rat models.1 Cell permeable
Uses
(1E,3E)- 1-(4-Fluorophenyl)-2-methyl-1-penten-3-one Oxime is a transient receptor potential ankyrin 1 (TRPA1) antagonist and has been investigated as potential analgesic drug for the treatment of chronic pain.
Uses
A-967079 has been used in blocking miR-711-induced TRPA1 (transient receptor potential cation channel subfamily A member 1) channel.
General Description
A-967079 prevents neuropathic and inflammatory pain. It reduces cold allodynia, which is produced by nerve injury.
Biochem/physiol Actions
A-967079 is a potent and selective antagonist of Transient Receptor Potential Anykrin 1 (TRPA1) with IC50′s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and minimal or no activity at other TRP channels or G-protein-coupled receptors, enzymes, transporters, and ion channels out of 89 tested. A-967079 blocks TRPA1 activation in human and rat cell lines and has been shown to reduce the responses of wide dynamic range (WDR) and nociceptive specific (NS) neurons to high-intensity mechanical stimulation.
References
1) McGaraughty et al. (2010), TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in uninjured, osteoarthritic, and inflamed rats; Mol. Pain, 6 14.
