Table 1.
Efficacy and potency of compounds 1–6 on TRPA1 channel and inhibitory (Inh.) effect on TRPM8 channel.
| Potency EC50 TRPA1 (μM) | Efficacy TRPA1 (% AITC 100 μM) | IC50 Inh. TRPA1 μM (AITC 100 μM) | IC50 Inh. TRPM8 μM (icilin 0.25 μM) | |
|---|---|---|---|---|
| Leucettamol A (1) | 3.7 ± 1.7 | 101.9 ± 12.4 | 4.7 ± 0.2 | 6.5 ± 0.3 |
| 2 | 9.4 ± 2.2 | 139.2 ± 7.5 | 11.6 ± 2.3 | 44.6 ± 10.1 |
| Leucettamol B (3) | 5.9 ± 1.9 | 103.3 ± 10.6 | 4.7 ± 0.9 | 6.4 ± 1.0 |
| 4 | 3.5 ± 2.5 | 109.6 ± 21.0 | 32.6 ± 4.8 | 65.7 ± 8.6 |
| 5 | 2.6 ± 0.1 | 69.2 ± 0.1 | 6.5 ± 0.4 | 6.5 ± 0.3 |
| 6 | 9.7 ± 3.3 | 100.0 ± 9.7 | 12.7 ± 0.8 | 29.0 ± 0.6 |