TABLE 2.
Potency and relative efficacy values for 5-HT2A-mediated intracellular Ca2+ release
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 | RSK2KO MEFs | F Test, p Value | WT MEFs | RSK2 KO MEFs | F Test, p Value | ||
| nM | % | ||||||
| 5-HT | 7.79 (8.11 ± 0.07) | 10.2 (7.99 ± 0.17) | 0.6969 | 97.0 ± 2.2 | 202 ± 12.5 | <0.0001 | 1.5 |
| DOI | 2.81 (8.55 ± 0.12) | 4.68 (8.33 ± 0.11) | 0.2309 | 87.3 ± 2.9 | 141 ± 4.6 | <0.0001 | 1.6 |
| Quipazine | 22.8 (7.64 ± 0.12) | 62.3 (7.21 ± 0.09) | 0.0114 | 88.1 ± 3.6 | 157 ± 5.7 | <0.0001 | 1.8 |
| 5-Methoxy-DMT | 60.0 (7.22 ± 0.08) | 58.2 (7.24 ± 0.14) | 0.9509 | 83.2 ± 2.6 | 145 ± 7.8 | <0.0001 | 1.7 |
| Lisuride | 985 (6.01 ± 0.17) | 1023 (5.99 ± 0.12) | 0.9405 | 29.1 ± 2.7 | 58.7 ± 3.8 | <0.0001 | 2.0 |
| m-CPP | 155 (6.81 ± 0.18) | 234 (6.63 ± 0.31) | 0.6959 | 60.5 ± 5.0 | 116 ± 17 | 0.0039 | 1.9 |
| SCH-23390 | 329 (6.48 ± 0.32) | 197 (6.71 ± 0.34) | 0.6864 | 25.7 ± 4.0 | 33.2 ± 5.2 | 0.2974 | 1.3 |
| α-Me-5-HT | 25.0 (7.60 ± 0.12) | 21.9 (7.66 ± 0.41) | 0.9401 | 106 ± 4.5 | 212 ± 32 | 0.0046 | 2.0 |
| MK212 | 817 (6.09 ± 0.18) | 846 (6.07 ± 0.33) | 0.9793 | 72.5 ± 7.8 | 168 ± 33 | 0.1035 | 2.3 |