Table 1. 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 βarr2 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 | 7.43 (3.54–12.9) | 100 (91–109) | 7.29 (3.50–12.7) | 87.1 (79.4–95.4) |
| serotonin | 7.62 (4.43–13.2) | 116 (107–126) | 7.24 (4.43–11.9) | 100 (93.9–108) |
| 23H-NBOMe | 33.6 (19.8–57.3) | 123 (115–131) | 33.7 (19.7–57.9) | 115 (107–123) |
| 24H-NBOMe | 3.88 (2.33–6.37) | 145 (136–154) | 3.89 (2.30–6.45) | 136 (127–145) |
| 25H-NBOMe | 11.4 (6.36–20.4) | 164 (151–180) | 11.0 (5.60–21.5) | 134 (121–148) |
| 26H-NBOMe | 8.70 (5.81–12.5) | 156 (147–165) | 8.74 (5.91–12.4) | 146 (138–154) |
| 34H-NBOMe | 248 (111–646) | 147 (129–182) | 238 (101–691) | 120 (104–152) |
| 35H-NBOMe | 343 (187–645) | 118 (107–135) | 310 (165–593) | 94.1 (83.8–108) |
| 30 min activation profiles | ||||
|---|---|---|---|---|
| reference agonist LSD |
reference agonist serotonin |
|||
| compound | EC50 (nM, CI) | Emax (%, CI) | EC50 (nM, CI) | Emax (%, CI) |
| LSD | 24.3 (ND) | 100 (91–110) | 23.8 (ND) | 79.4 (72.0–87.3) |
| serotonin | 11.5 (7.13–18.9) | 128 (119–139) | 10.9 (7.60–15.8) | 100 (94.8–106) |
| 23H-NBOMe | 74.4 (55.8–95.9) | 133 (128–139) | 74.5 (53.9–98.8) | 114 (109–119) |
| 24H-NBOMe | 8.34 (6.11–11.1) | 154 (147–161) | 8.32 (5.85–11.5) | 132 (125–139) |
| 25H-NBOMe | 24.3 (13.4–45.0) | 179 (163–199) | 22.9 (12.8–41.8) | 130 (118–143) |
| 26H-NBOMe | 16.3 (13.0–20.8) | 165 (159–172) | 16.4 (12.4–22.0) | 142 (135–149) |
| 34H-NBOMe | 488 (226–1707) | 162 (142–218) | 458 (191–2287) | 118 (101–171) |
| 35H-NBOMe | 678 (385–1295) | 137 (123–162) | 625 (353–1148) | 98.5 (88.8–115) |