Summary of the activity of TRPA1 agonists in HEK293 cells transiently expressing TRPA1 and TRPA1-M4, and in untrasfected cells
Values are the mean ± S.D. of nonlinear least-squares fit parameters for n = 3 to 5 concentration-response experiments. Maximal response is the ratio of the high-concentration response relative to the response of HEK293-TRPA1 to 100 μM FTS.
Agonist | TRPA1 | TRPA1 Mutant | HEK-WT | ||||||
|---|---|---|---|---|---|---|---|---|---|
| EC50 | Maximal Response | EC50 | Maximal Response | EC50 | Maximal Response | ||||
| μM | μM | μM | |||||||
| AITC | 5 ± 2 | 0.77 | — | — | — | — | |||
| FTS | 7 ± 4 | 1.3 ± 0.1 | 11 ± 5 | 0.95 ± 0.04 | — | — | |||
| FTA | 100 ± 40 | 1.0 ± 0.1 | 160 ± 40 | 0.9 ± 0.2 | — | — | |||
| Disulfiram | 3 ± 2 | 0.8 ± 0.1 | — | — | — | — | |||
| Chlordantoin | 3 ± 1 | 0.9 ± 0.1 | 30 ± 10 | 0.43 ± 0.07 | — | — | |||
| 15d-PGJ2 | 22 ± 7 | 1.2 ± 0.1 | 210 ± 70 | 1.2 ± 0.2 | 300a | N.D. | |||
| ETYA | 4a | N.D. | 25a | N.D. | 25a | N.D. | |||
<20% response at the highest concentration tested; N.D., not determined.
↵ a Could not be fit accurately with a Hill function. Instead of an EC50 value, the threshold concentration (i.e., the average concentration required to increase the normalized response by 20%) is provided for this compound.