A-967079

Использование

(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.

Общее описание

A-967079 prevents neuropathic and inflammatory pain. It reduces cold allodynia, which is produced by nerve injury.

Биохимия/физиол Действия

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.