Table 1.
Affinity of substituted phenethylamines and other compounds for recombinant 5-HT1A, 5-HT2A, 5-HT2B and 5-HT2C receptors.
| Inhibition of radioligand binding Ki mean ± sem (nM) (n) | Selectivity (binding ratios) | ||||||
|---|---|---|---|---|---|---|---|
| Drug | 5-HT1A [3H]8OH-DPAT | 5-HT2A [125I]DOI | 5-HT2B [3H]5-HT | 5-HT2C [125I]DOI | 5-HT2A : 5-HT1A | 5-HT2A : 5-HT2B | 5-HT2A : 5-HT2C |
| 25D-NBOMe | 4510 ± 730 (3) | 0.22 ± 0.026 (5) | 2.05 ± 0.49 (3) | 0.69 ± 0.02 (4) | 20500 | 9.3 | 3.1 |
| 25E-NBOMe | 1680 ± 350 (3) | 0.127 ± 0.019 (5) | 1.11 ± 0.32 (3) | 0.311 ± 0.071 (4) | 13200 | 8.7 | 2.4 |
| 25H-NBOMe | 4520 ± 3+0 (3) | 4.9 ± 1.3 (5) | 62.9 ± 7.5 (3) | 16.4 ± 5.0 (6) | 920 | 13 | 3.3 |
| 25I-NBOH | 2220 ± 590 (3) | 0.169 ± 0.013 (5) | 1.91 ± 0.48 (6) | 1.03 ± 0.24 (4) | 13100 | 11 | 6.1 |
| 25N-NBOMe | 2260 ± 230 (3) | 0.144 ± 0.042 (5) | 8.7 ± 1.6 (3) | 1.06 ± 0.35 (4) | 15700 | 60 | 7.4 |
| 5-HT | 1.71 ± 0.24 (4) | 16.8 ± 2.2 (3) | 6.31 ± 0.94 (4) | 2.52 ± 0.45 (7) | 0.10 | 0.38 | 0.15 |
| LSD | 1.22 ± 0.23 (4) | 0.091 ± 0.044 (3) | 0.57 ± 0.14 (3) | 1.60 ± 0.27 (4) | 13.4 | 6.3 | 17.6 |
| DOM | 3660 ± 470 (4) | 18.3 ± 1.7 (4) | 41.0 ± 5.9 (3) | 18.9 ± 2.4 (4) | 200 | 2.2 | 1.0 |
(n) Number of independent experiments conducted in duplicate.
Binding Hill slopes for h5-HT1A [3H]8-OH-DPAT ranged from -0.58 to -0.90, for h5-HT2A [125I]DOI ranged from -0.32 to -1.78, for h5-HT2B [3H]5-HT ranged from -0.87 to -1.17 and for h5-HT2C [125I]DOI ranged from -0.58 to -0.96.