Effect of different compounds used in the study on distinct modes of rat TRPV1 activation
Since putative endogenous ligands are weak agonists, activation by anandamide and NADA was evaluated at sensitizing pH conditions (pH 6). The IC50 values shown are in nanomolar.
AMG8163 | AMG8563 | AMG8562 | AMG7905 | |
|---|---|---|---|---|
| Capsaicin | 0.6 ± 0.3 | 2.9 ± 0.49 | 1.75 ± 0.48 | 39 ± 17 |
| Anandamide | 1.79 ± 0.68 | 3.97 ± 2. | 9.29 ± 1.4 | 6.26 ± 2.6 |
| NADA | 2.36 ± 1.5 | 6.37 ± 0.9 | 3.87 ± 1.8 | 4101 ± 1412 |
| pH 5 | 0.59 ± 0.3 | >4000 | Potentiator | Potentiator |
| Heat | 0.15 ± 0.1 | 1.46 ± N.A. | >4000 | Potentiator |
N.A., not available.