Overview
- Eid, S.R. et al. (2008) Mol. Pain 4, 48.
Alomone Labs HC-030031 inhibits TRPA1 currents induced by AITC in HEK-293 cells.Dose-response curve of HC-030031 (#H-105) inhibition of human TRPA1-mediated increase in intracellular Ca2+. Cells were loaded with Calcium 5 dye, incubated for 10 min with HC-030031, and stimulated by 1 µM allyl isothiocyanate. Changes in intracellular Ca2+ following stimulation were detected as changes in maximum relative fluorescence (RFU). IC50 was determined at 13.8 µM.
HC-030031 is a selective small molecule that acts as a TRPA1 channel blocker. It was used to evaluate the role of TRPA1 receptors in models of inflammatory and neuropathic pain, and in tests of acute heat sensitivity and motor coordination1.
Transient receptor potential ankyrin subfamily, member 1 (TRPA1) is a non-selective cation channel originally characterized as a noxious cold-activated ion channel. Several studies have showed that a large number of pungent and irritant compounds can activate TRPA1 channel. It has been suggested that TRPA1 may be involved in the normal detection of pain.
HC-030031 has the ability to attenuate the mechanical hypersensitivity in rats 6 weeks post surgery and in other models of chronic inflammatory and neuropathic pain1,2.
Intraperitoneal injection of HC-030031 was shown to inhibit AITC and formalin-evoked TRPA1 currents in vitro, and inhibit AITC and formalin-induced nociceptive behaviors in vivo1.
Several studies have shown that HC-030031 interferes with glucose tolerance independently of TRPA13. It has an IC50 value of 4.9 μM1.
