Table 1. Comparison of ligand activation of wildtype and mutant mTRPV1 channels by capaicin analogs.
Cap | Cap-1 | Cap+1 | ||||||||
---|---|---|---|---|---|---|---|---|---|---|
EC50 (µM) | K | N | EC50 (µM) | K | N | EC50 (µM) | K | N | ||
WT | 0.14 ± 0.01 | 1.82 ± 0.22 | 4 | 0.10 ± 0.01 | 1.20 ± 0.05 | 3 | 4.31 ± 0.23* | 1.44 ± 0.11 | 4 | |
T551V | 1.56 ± 0.20† | 1.74 ± 0.13 | 5 | 9.13 ± 1.10*‡ | 1.83 ± 0.31 | 5 | 70.12 ± 7.74*§ | 1.71 ± 0.10 | 8 | |
E571A | 1.53 ± 0.10† | 1.86 ± 0.07 | 4 | 19.31 ± 0.22*‡ | 2.01 ± 0.02 | 6 | 31.43 ± 0.02*§ | 1.84 ± 0.11 | 6 | |
I574A | 0.22 ± 0.02† | 1.41 ± 0.12 | 3 | 2.80 ± 0.11*‡ | 1.35 ± 0.23 | 7 | 10.73 ± 0.33*§ | 1.98 ± 0.12 | 5 | |
T671S | 0.05 ± 0.06 | 0.87 ± 0.11 | 3 | 22.80 ± 0.40*‡ | 4.94 ± 0.30 | 3 | 35.29 ± 1.19*§ | 3.16 ± 0.45 | 3 | |
Y512F | 1.12 ± 0.17† | 1.35 ± 0.08 | 4 | 25.18 ± 1.18*‡ | 2.68 ± 0.34 | 3 | 99.48 ± 6.82*§ | 1.46 ± 0.17 | 3 |
* Compared to Capsaicin (Cap).
†Compared to WT Cap.
‡Compared to WT Cap-1.
§Compared to WT Cap+1.
EC50, half maximal effective concentration; K, Hill coefficient; N, number of patches.