Potency and relative efficacy values for 5-HT2A-mediated ERK1/2 phosphorylation
Agonist potencies (EC50) and relative efficacies (Emax) represent the average of four to five independent experiments. pEC50 values are represented as −log of EC50, given as molar values.
| Agonist | Agonist Potency EC50 (pEC50 ± S.E.M.) | Relative Agonist Efficacy Emax ± S.E.M. | EmaxRSK2KO/EmaxWT | ||||
|---|---|---|---|---|---|---|---|
| WT MEFs | RSK2 KO MEFs | F Test p Value | WT MEFs | RSK2 KO MEFs | F Test p Value | ||
| nM | % | ||||||
| 5-HT | 6.51 (8.19 ± 0.08) | 3.92 (8.41 ± 0.11) | 0.4729 | 99.1 ± 3.5 | 325 ± 15 | <0.0001 | 3.3 |
| DOI | 0.370 (9.43 ± 0.16) | 0.889 (9.05 ± 0.22) | 0.4866 | 99.0 ± 3.9 | 348 ± 24 | <0.0001 | 3.5 |
| Quipazine | 2.42 (8.62 ± 0.17) | 4.24 (8.37 ± 0.20) | 0.4796 | 108 ± 7 | 270 ± 22 | <0.0001 | 2.5 |
| 5-Methoxy-DMT | 8.23 (8.08 ± 0.19) | 7.45 (8.13 ± 0.19) | 0.9356 | 89.8 ± 7.7 | 343 ± 29 | <0.0001 | 3.8 |
| Lisuride | 7.39 (8.13 ± 0.21) | 2.27 (8.64 ± 0.32) | 0.5414 | 90.9 ± 8.3 | 278 ± 32 | 0.0010 | 3.1 |
| m-CPP | 21.6 (7.67 ± 0.18) | 21.6 (7.67 ± 0.19) | 0.9976 | 105 ± 9 | 245 ± 25 | <0.0001 | 2.3 |
| SCH-23390 | 21.2 (7.67 ± 0.29) | 3.65 (8.44 ± 0.23) | 0.3295 | 51.3 ± 7.4 | 202 ± 19 | 0.0100 | 3.9 |
| α-Me5-HT | 3.07 (8.51 ± 0.19) | 3.91 (8.41 ± 0.17) | 0.8488 | 83.4 ± 6.3 | 327 ± 23 | <0.0001 | 3.9 |
| MK212 | 133 (6.88 ± 0.13) | 42.5 (7.37 ± 0.14) | 0.2023 | 71.2 ± 4.6 | 261 ± 18 | 0.0005 | 3.7 |