Table 2. Summary of the Potency (EC50) and Efficacy (Emax, Where the Emax of Either Serotonin or LSD is Set to 100%) Values of All the Tested Compounds in the miniGαq Recruitment Assay, Calculated Using Either the Full 120 Min or the First 30 Min Activation Profilesa.
| 120 min activation profiles | ||||
|---|---|---|---|---|
| reference agonist LSD |
reference agonist serotonin |
|||
| compound | EC50 (nM, CI) | Emax (%, CI) | EC50 (nM, CI) | Emax (%, CI) |
| LSD | 7.40 (1.82–17.7) | 100 (84–115) | 7.23 (1.73–17.5) | 39.6 (33.7–46.0) |
| serotonin | 66.4 (35.5–151) | 256 (230–301) | 63.5 (33.9–143) | 103 (92.5–121) |
| 23H-NBOMe | 147 (71.8–436) | 81.2 (70–102) | 146 (73.8–408) | 31.9 (27.5–39.6) |
| 24H-NBOMe | 22.1 (12.1–42.1) | 144 (129–161) | 22.2 (12.4–41.6) | 56.9 (51.2–63.4) |
| 25H-NBOMe | 49.6 (27.2–84.8) | 141 (128–155) | 49.2 (26.6–85.4) | 58.8 (53.3–64.9) |
| 26H-NBOMe | 40.9 (23.7–68.2) | 136 (124–148) | 40.9 (23.9–67.7) | 53.3 (48.8–58.2) |
| 34H-NBOMe | 974 (ND) | 134 (ND) | 947 (ND) | 55.3 (45.6–297) |
| 35H-NBOMe | 1097 (ND) | 89.1 (74–219) | 1087 (ND) | 37.1 (30.5–112) |
| 30 min activation profiles | ||||
|---|---|---|---|---|
| reference
agonist LSD |
reference agonist serotonin |
|||
| compound | EC50 (nM, CI) | Emax (%, CI) | EC50 (nM, CI) | Emax (%, CI) |
| LSD | 17.7 (10.1–38.6) | 98.2 (85–114) | 16.3 (8.59–38.7) | 31.9 (27.4–37.2) |
| serotonin | 88.5 (46.1–213) | 305 (272–365) | 62.2 (22.5–269) | 87.9 (74.4–121) |
| 23H-NBOMe | 236 (ND) | 89.6 (75–112) | 191 (ND) | 27.1 (22.6–33.3) |
| 24H-NBOMe | 37.4 (20.6–66.4) | 171 (155–189) | 35.1 (17.5–68.7) | 54.3 (48.5–61.2) |
| 25H-NBOMe | 86.2 (57.0–124) | 181 (167–196) | 129 (69.2–263) | 74.8 (65.6–88.8) |
| 26H-NBOMe | 68.0 (38.6–115) | 162 (147–181) | 68.3 (34.0–129) | 51.9 (46.0–59.4) |
| 34H-NBOMe | 1321 (629–33 780) | 156 (130–340) | 1334 (ND) | 51.8 (ND) |
| 35H-NBOMe | 1393 (ND) | 107 (94–163) | 1296 (683–10 760) | 48.3 (41.0–83.6) |
a
Data are from three independent experiments. CI: 95% confidence interval. ND: confidence interval not determined.