Table 4. Functional Activity at Human 5-HT2B and 5-HT2C Receptors in Cellular Assaysa.
| potency and efficacy—cells |
||
|---|---|---|
| calcium mobilization h5-HT2B | calcium mobilization h5-HT2C | |
| ligand | EC50 (nM) Emax(% 5-HT) | EC50 (nM) Emax(% 5-HT) |
| norpsilocin | 13 | 32 |
| (12–15) | (28–37) | |
| Emax = 82 | Emax = 96 | |
| 4-AcO-NMT | 153 | 296 |
| (135–173) | (254–345) | |
| Emax = 74 | Emax = 84 | |
| psilocin | 8 | 34 |
| (7–10) | (28–40) | |
| Emax = 38 | Emax = 84 | |
| psilocybin | 612 | 3,741 |
| (504–743) | (3,120–4,486) | |
| Emax = 38 | Emax = 88 | |
| psilacetin | 88 | 408 |
| (69–114) | (318–525) | |
| Emax = 29 | Emax = 32 | |
| 4-HO-TMT | 845 | 8,940 |
| (675–1,059) | (7,592–10,520) | |
| Emax = 32 | Emax = 64 | |
a
Potency (EC50) with 95% CI values (parentheses) and maximum efficacy (Emax) for each are listed. Reference compound 5-HT displayed potency values of 0.9 nM (0.7–1.1) and 0.4 nM (0.3–0.5) at 5-HT2B and 5-HT2C, respectively.