Table 2.
Potency and efficacy of substituted phenethylamines and other compounds at recombinant 5-HT1A, 5-HT2A and 5-HT2C receptors.
| Drug | EC50 mean ± sem (nM) (n) % maximum stimulation ± sem* | Selectivity (functional ratios) | |||||
|---|---|---|---|---|---|---|---|
| 5-HT1A Stimulation of [35S]GTPγS binding | 5-HT2A Stimulation of IP-1 formation | 5-HT2B Stimulation of IP-1 formation | 5-HT2C Stimulation of IP-1 formation | 5-HT2A: 5-HT1A | 5-HT2A: 5-HT2B | 5-HT2A: 5-HT2C | |
| 25D-NBOMe | 5900 ± 1900 (4) 55 ± 20% | 1.53 ± 0.10 (3) 95.1 ± 6.8% | 32.3 ± 6.8 (4) 47.7 ± 8.1% | 1.37 ± 0.36 (3) 96.1 ± 2.5% | 3900 | 21 | 0.90 |
| 25E-NBOMe | 13700 ± 5600 (6) 38.0 ± 6.2% | 0.50 ± 0.14 (4) 87.1 ± 6.6% | 23.5 ± 6.0 (5) 49.4 ± 6.8% | 0.95 ± 0.18 (3) 91.8 ± 4.4% | 27,000 | 47 | 1.9 |
| 25H-NBOMe | 28400 ± 8600 (4) 52 ± 14% | 40.7 ± 8.1 (4) 85.9 ± 1.7% | 463 ± 71 (4) 37.7 ± 9.0% | 13.8 ± 2.6 (3) 95.5 ± 3.0% | 700 | 11 | 0.34 |
| 25I-NBOH | 37000 ± 13000 (3) 74 ± 18% | 0.76 ± 0.26 (4) 87.5 ± 4.1% | 111 ± 13 (4) 21.3 ± 8.3% | 2.38 ± 0.72 (3) 94.0 ± 4.0% | 49,000 | 146 | 3.1 |
| 25N-NBOMe | 4800 ± 1800 (5) 35.6 ± 6.6% | 0.51 ± 0.19 (3) 87.9 ± 3.4% | 47 ± 11 (4) 57.6 ± 8.6% | 1.32 ± 0.27 (3) 99.4 ± 0.4% | 9400 | 92 | 2.6 |
| 5-HT | 2.88 ± 0.61 (6) 94.7 ± 3.6% | 19.4 ± 3.7 (8) 98.7 ± 2.7% | 6.3 ± 1.2 (5) 100.2 ± 2.8% | 2.8 ± 1.0 (6) 98.9 ± 3.3% | 0.15 | 0.32 | 0.14 |
| LSD | 1.31 ± 0.46 (3) 93.2 ± 6.4% | 0.706 ± 0.065 (3) 64.5 ± 6.3% | 3.07 ± 0.65 (6) 23.3 ± 4.9% | 1.74 ± 0.29 (3) 92.5 ± 4.8% | 1.9 | 4.3 | 2.5 |
| DOM | 12800 ± 4700 (3) 74 ± 25% | 39.9 ± 5.4 (3) 94.6 ± 4.1% | 145 ± 47 (4) 96.2 ± 3.2% | 21.9 ± 5.9 (3) 96.0 ± 4.0% | 320 | 3.6 | 0.55 |
(n) Number of independent experiments conducted in duplicate.
*
Drug-induced stimulation is normalized to the maximal stimulation by 5-HT.