A-967079

A-967079 is a potent, selective, and orally bioavailable inhibitor of the TRPA1 (Transient Receptor Potential Ankyrin 1) channel. It has IC50 values of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively. The compound displays 1000-fold selectivity for TRPA1 over other TRP channels and is >150-fold selective over 75 other ion channels, enzymes, and G-protein-coupled receptors. Developed by Abbott Laboratories, A-967079 was initially investigated for pain disorders. Oral administration produces robust drug exposure in rodents and exhibits analgesic efficacy in allyl isothiocyanate-induced nocifensive response and osteoarthritic pain in rats. It attenuates cold allodynia produced by nerve injury but does not alter noxious cold sensation in naive animals, suggesting distinct roles of TRPA1 in physiological and pathological states. Unlike TRPV1 antagonists, A-967079 does not alter body temperature and does not produce locomotor or cardiovascular side effects. More recently, A-967079 has shown promise as an antiviral agent against Enterovirus D68 (EV-D68), demonstrating potent and broad-spectrum antiviral activity with a high selectivity index against multiple strains of the virus. It has also been investigated as a potential antidote for toxic inhalation hazards.

Other names

(1E,3E)-1-(4-Fluorophenyl)-2-methyl-1-pentene-3-one oxime1-Penten-3-one, 1-(4-fluorophenyl)-2-methyl-, oxime, (1E,3E)-