Table 1.
Receptor binding data for 5-MeO-DMT and α,α,β,β-tetradeutero-5-MeO-DMT
| Receptor | Radioligand | Speciesa | 5-MeO-DMT Ki nM (±SEM)b | α,α,β,β-Tetradeutero-5-MeO-DMT Ki nM (±SEM)b |
|---|---|---|---|---|
| 5-HT1A | [3H]8-OH-DPAT | Human | 3.0 (0.2) | 3.0 (0.4) |
| 5-HT1B | [3H]GR125743 | Human | 14.0 (2) | 3.5 (0.6) |
| 5-HT1D | [3H]GR125743 | Human | 2.3 (0.3) | 1.7 (0.3) |
| 5-HT1E | [3H]5-HT | Human | 376 (67) | 483 (90) |
| 5-HT2A | [3H]ketanserin | Human | 907 (170) | 1292 (243) |
| 5-HT2B | [3H]LSD | Human | 36 (6) | 90 (14) |
| 5-HT2C | [3H]mesulergine | Rat | 418 (35) | 286 (25) |
| 5-HT5A | [3H]LSD | Human | 505 (72) | 151 (20) |
| 5-HT6 | [3H]LSD | Human | 6.5 (1.2) | 10.0 (1) |
| 5-HT7 | [3H]LSD | Human | 4.5 (0.5) | 2.6 (0.4) |
| α1A | [3H]prazocin | Human | 4373 (354) | 1013 (92) |
| α1B | [3H]prazocin | Human | 2188 (219) | 841 (67) |
| α1D | [125I]HEAT | Human | 439 (52) | 202 (17) |
| α2A | [3H]clonidine | Human | 938 (56) | 1871 (187) |
| α2B | [3H]clonidine | Human | 430 (40) | 513 (48) |
| α2C | [3H]clonidine | Human | 206 (14) | 274 (16) |
| β2 | [3H]CGP12177 | Human | 2679 (238) | 4560 (365) |
| D3 | [3H]N-methyl-spiperone | Rat | > 10000 | 7087 (1125) |
| H1 | [3H]pyrilamine | Human | 7580 (1024) | > 10000 |
| H2 | [3H]tiotidine | Human | > 10000 | 7165 (853) |
| SERT | [3H]citalopram | Human | 3603 (559) | 2761 (330) |
| Sigma-2 | [3H]DTG | Rat | 3689 (336) | 7171 (1156) |
a
The experiments were performed using cloned receptors.
b
5-MeO-DMT and α,α,β,β-tetradeutero-5-MeO-DMT bound to the following sites with Ki values > 10,000 nM: 5-HT3, rat brain benzodiazepine site, Ca2+ channels, D1, D2, D4, D5, DAT, NET, β1, β3, DOR, MOR, KOR, EP3, EP4, GABAA, H3, H4, M1, M2, M3, M4, M5, and sigma-1.