Overview
- Klionsky, L. et al. (2007) Mol. Pain 3, 39.
- Miller, S. et al. (2014) PLoS ONE 9, e107151.
Alomone Labs AMG-9090 inhibits TRPA1 channel currents in HEK-293 cells.Dose-response curve of AMG-9090 (#A-300) inhibition of human TRPA1-mediated increase in intracellular Ca2+. Cells were loaded with Calcium 5 dye, incubated for 10 min with AMG-9090, and stimulated by 1 µM allyl isothiocyanate (EC80). Changes in intracellular Ca2+ following stimulation were detected as changes in maximum relative fluorescence (RFU). IC50 was determined at 0.527 nM.
AMG-9090 is a small synthetic molecule that acts as a TRPA1 channel blocker. AMG-9090 was shown to inhibit intracellular calcium increase mediated by human TRPA1 channels in Chinese hamster ovary cells with IC50 values of 21 nM1. The compound also possesses inhibitory effects on human TRPM8 and TRPV1 channels1,2.
TRPA1 channels are non-selective cation channels expressed in the small neurons of the dorsal root and trigeminal ganglia. They play an important role in models of inflammatory and neuropathic pain and have the ability to detect pungent or irritant compounds.
Studies have shown that blockade of TRPA1 channels may help in migraine attack and can be used as a possible new target for its treatment. Also, evidence shows that TRPA1 blockers could serve as novel therapeutic strategies for chemotherapeutic induced peripheral neuropathy1,3.
