Chemical Name: (1E,3E)-1-(4-Fluorophenyl)-2-methyl-1-pentene-3-one oxime
Biological ActivityA 967079 (also known as A-079) is a selective TRPA1 channel blocker (IC50 values are 67 and 289 nM at human and rat TRPA1 receptors respectively) that 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. A 967079 exhibits analgesic effects in a rat osteoarthritic pain model.
External Portal InformationThe Chemical Probes pages of the Structural Genomics Consortium website are a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of A 967079 (A-079) is reviewed.
The technical data provided above is for guidance only.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in uninjured, osteoarthritic, and inflamed rats.
McGaraughty et al.
Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation.
Chen et al.
Citations for A 967079
The citations listed below are publications that use Tocris products. Selected citations for A 967079 include:
7 Citations: Showing 1 - 7
Irritant-evoked activation and calcium modulation of the TRPA1 receptor.
Authors: Zhao Et al.
The role of Nav1.7 and methylglyoxal-mediated activation of TRPA1 in itch and hypoalgesia in a murine model of type 1 diabetes.
Authors: Cheng Et al.
A critical evaluation of TRPA1-mediated locomotor behavior in zebrafish as a screening tool for novel anti-nociceptive drug discovery.
Authors: Ko Et al.
Sci Rep 2019;9:2430
ROS/TRPA1/CGRP signaling mediates cortical spreading depression.
Authors: Jiang Et al.
J Headache Pain 2019;20:25
Ethyl Vanillin Activates TRPA1.
Authors: Wu Et al.
J Pharmacol Exp Ther 2017;362:368
Structure of the TRPA1 ion channel suggests regulatory mechanisms.
Authors: Paulsen Et al.
Inhibitory Interneurons That Express GFP in the PrP-GFP Mouse Spinal Cord Are Morphologically Heterogeneous, Innervated by Several Classes of Primary Afferent and Include Lamina I Projection Neurons among Their Postsynaptic Targets.
Authors: Ganley Et al.
Mol Brain 2015;35:7626
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A967079 was used in the animal behavior test to block the TRPA1-mediated chronic itch at the concentration of 10mg/Kg