Table 1 IC 50 values of TRPM8 antagonists at different TRP channels activated by specific agonists. Values shown are in nanomolar except where indicated with * are shown in μM. NA = not available
Antagonist | TRPM8 Menthol (Cold) | TRPA1 (AITC) | TRPV1 (Capsaicin) | TRPV3 2-APB | TRPV4 (4αPDD) |
|---|---|---|---|---|---|
AMG8788 | 63.2 ± 31.7 (16 ± 14) | 1 ± 0.7* | >20* | >20* | >20* |
AMG0635 | 57.2 ± 0.1 (5.5 ± 3.4) | 4.5 ± 1.6* | >20* | >20* | >20* |
AMG9678 | 31.2 ± 8.3 (6.2 ± 1.9) | 0.6 ± 0.4* | >20* | >20* | >20* |
Compound 496 | 25.8 ± 6.6 (12 ± 0.9) | 5.6 ± 2.4* | 4.3* | >10* | >10* |
AMG2850 | 156 ± 110 (7.3 ± NA) | >20* | >10* | >10* | >10* |