Overview
- Petrus, M. et al. (2007) Mol. Pain 3, 40.
Alomone Labs AP-18 inhibits allyl isothiocyanate-induced Ca2+ signal in TRPA1 expressing cells.Dose-response curve for the inhibition of human TRPA1 expressing HEK-293 cells that were loaded with Calcium 5 dye for changes in intracellular Ca2+ measurements. Allyl isothiocyanate (100 µM)-induced Ca2+ signal was inhibited by 5, 50 and 100 µM AP-18 (#A-250), with estimated IC50 of 12 µM.
The transient receptor potential (TRP) channel is one of the largest families of cation channels1. TRPA1 is expressed in sensory and nociceptive neurons and has a significant role in inflammatory responses. Bradykinin and histamine receptors induce TRPA1 activity. A study conducted found that TRPA1 deficient mice did not develop an elevated mechanical and thermal pain response following bradykinin injection, suggesting that TRPA1 has a vital role in bradykinin signaling pathways2.
TRPA1 also plays a role in acute and chronic respiratory disease pathophysiology. Prolonged exposure to TRPA1 agonists such as chlorine and aldehydes can cause reactive airways dysfunction syndrome characterized by symptoms such as wheezing, coughing and dyspnea. In light of this, TRPA1 may be a target for airway anti-inflammatory research3.
AP-18 is a reversible TRPA1 blocker with an IC50 value of 3.1 and 4.5 μM for human and rat TRPA1 channels respectively.
