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. 2016 Jun 1;6:26894. doi: 10.1038/srep26894

Figure 5. Compounds 16-8 and 16-19 also potently inhibit TRPA1, not TRPV1-3.

Figure 5

(A) Specificity vs TRPV1-3. Both 16-8 and 16-19 (5 μM each) compounds did not inhibit TRPV1, −2 or −3 channels (all mouse isoforms), directed over-expression in N2a cells and subsequent Ca++ imaging. Mean±SEM is shown, ≥100 cells per condition. (B) Dose-dependent inhibition of TRPA1 (mouse, directed expression in N2a cells) by GSK 205, 16-8 and 16-19, activation with 100 μM mustard oil, resulting in IC50 of 5.56 ± 0.4 μM (GSK205), 0.41 ± 0.37 μM (16-19), 0.43 ± 0.3 μM (16-8). Plot generated from averaged peak ∆Ca++ concentration of ≥75 cells per data-point.