A-967079 Explained
A-967079 is a drug which acts as a potent and selective antagonist for the TRPA1 receptor. It has analgesic and antiinflammatory effects and is used in scientific research, but has not been developed for medical use.[1] [2] [3] [4] [5]
Notes and References
- Chen J, Joshi SK, DiDomenico S, Perner RJ, Mikusa JP, Gauvin DM, Segreti JA, Han P, Zhang XF, Niforatos W, Bianchi BR, Baker SJ, Zhong C, Simler GH, McDonald HA, Schmidt RG, McGaraughty SP, Chu KL, Faltynek CR, Kort ME, Reilly RM, Kym PR . 6 . Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation . Pain . 152 . 5 . 1165–72 . May 2011 . 21402443 . 10.1016/j.pain.2011.01.049 . 21881155 .
- Wei H, Karimaa M, Korjamo T, Koivisto A, Pertovaara A . Transient receptor potential ankyrin 1 ion channel contributes to guarding pain and mechanical hypersensitivity in a rat model of postoperative pain . Anesthesiology . 117 . 1 . 137–48 . July 2012 . 22588108 . 10.1097/ALN.0b013e31825adb0e . 287826 . free .
- Banzawa N, Saito S, Imagawa T, Kashio M, Takahashi K, Tominaga M, Ohta T . Molecular basis determining inhibition/activation of nociceptive receptor TRPA1 protein: a single amino acid dictates species-specific actions of the most potent mammalian TRPA1 antagonist . The Journal of Biological Chemistry . 289 . 46 . 31927–39 . November 2014 . 25271161 . 10.1074/jbc.M114.586891 . 4231671 . free .
- Koivisto A, Chapman H, Jalava N, Korjamo T, Saarnilehto M, Lindstedt K, Pertovaara A . TRPA1: a transducer and amplifier of pain and inflammation . Basic & Clinical Pharmacology & Toxicology . 114 . 1 . 50–5 . January 2014 . 24102997 . 10.1111/bcpt.12138 . free .
- Achanta S, Chintagari NR, Brackmann M, Balakrishna S, Jordt SE . TRPA1 and CGRP antagonists counteract vesicant-induced skin injury and inflammation . Toxicology Letters . 293 . 140–148 . September 2018 . 29535050 . 10.1016/j.toxlet.2018.03.007 . 5975083 .