TABLE 1.
Potency and relative efficacy values for 5-HT2A-mediated IP accumulation
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 | 134 (6.87 ± 0.03) | 57.8 (7.24 ± 0.11) | 0.0309 | 99.1 ± 1.2 | 209 ± 8.5 | <0.0001 | 2.1 |
| DOI | 12.4 (7.91 ± 0.10) | 8.51 (8.07 ± 0.10) | 0.7145 | 71.7 ± 2.4 | 211 ± 13 | <0.0001 | 2.9 |
| Quipazine | 188 (6.73 ± 0.09) | 140 (6.85 ± 0.15) | 0.7010 | 82.7 ± 2.9 | 220 ± 14 | <0.0001 | 2.7 |
| 5-Methoxy-DMT | 590 (6.23 ± 0.13) | 386 (6.41 ± 0.15) | 0.6487 | 66.6 ± 4.0 | 224 ± 14 | <0.0001 | 3.4 |
| Lisuride | 3.52 (8.45 ± 0.57) | 5.99 (8.22 ± 0.20) | 0.7450 | 17.1 ± 2.6 | 63.1 ± 3.8 | <0.0001 | 3.7 |
| m-CPP | 167 (6.78 ± 0.19) | 231 (6.64 ± 0.09) | 0.5364 | 27.8 ± 2.4 | 90.0 ± 3.6 | <0.0001 | 3.2 |
| SCH-23390 | 16.3 (7.79 ± 0.30) | 24.6 (7.61 ± 0.08) | 0.5342 | 14.0 ± 1.5 | 33.9 ± 1.1 | <0.0001 | 2.4 |
| α-Me-5-HT | 178 (6.75 ± 0.04) | 68.9 (7.16 ± 0.05) | <0.0001 | 95.4 ± 1.9 | 134 ± 3.0 | <0.0001 | 1.4 |
| MK212 | 3390 (5.47 ± 0.09) | 2330 (5.63 ± 0.05) | 0.1148 | 80.4 ± 5.7 | 152 ± 5.0 | <0.0001 | 1.9 |