Table 1.
Binding affinity, activation potency, and activation efficacy of 2C and NBOMe drugs on 5-HT receptors (adapted from [25]).
|
Drug / Receptor |
5-HT1A | 5-HT2A | 5-HT2B | 5-HT2C | Model |
|---|---|---|---|---|---|
|
Receptor Binding Ki (nM) |
|||||
| 2C-B | 240 | 8.6 | - | 47 | HEK293 cells expressing human 5-HT1A, 5-HT2A and 5-HT2C receptors |
| 2C‐T‐7 | 520 | 6.5 | - | 39 | |
| 25B-NBOMe | 3600 | 0.5 | - | 6.2 | |
| 25T7-NBOMe | 1800 | 1.1 | - | 6.4 | |
| LSD | 3 | 4.2 | - | 15 | |
|
Activation potency EC50 (nM) |
|||||
| 2C-B | - | 80 | 130 | - | NIH-3T3 and HEK293 cells expressing human 5-HT2A and 5-HT2B receptors, respectively |
| 2C‐T‐7 | - | 130 | 350 | - | |
| 25B-NBOMe | - | 40 | 10 | - | |
| 25T7-NBOMe | - | 260 | 310 | - | |
| LSD | - | 260 | 12,000 | - | |
|
Activation efficacy % maximum |
|||||
| 2C-B | - | 45 | 89 | - | |
| 2C‐T‐7 | - | 76 | 45 | - | |
| 25B-NBOMe | - | 28 | 19 | - | |
| 25T7-NBOMe | - | 41 | 14 | - | |
| LSD | - | 28 | 71 | - | |