Table 1. Affinities of Psilocybin Analogues in Radioligand Binding Assays for Human 5-HT Receptorsa.
| 5-HT1A | 5-HT1B | 5-HT1D | 5-ht1e | 5-HT2A | 5-HT2B | 5-HT2C | 5-HT5A | 5-HT6 | 5-HT7a | |
|---|---|---|---|---|---|---|---|---|---|---|
| Drug | Ki (nM) | Ki (nM) | Ki (nM) | Ki (nM) | Ki (nM) | Ki (nM) | Ki (nM) | Ki (nM) | Ki (nM) | Ki (nM) |
| norpsilocin | 86 | 99 | 194 | 161 | 391 | 57 | 243 | 365 | 54 | 68 |
| baeocystin | 370 | 394 | 1,352 | 134 | 117 | |||||
| 4-AcO-NMT | 141 | 994 | 150 | 522 | 1,512 | 76 | 729 | 389 | 82 | 1,766 |
| psilocin | 164 | 580 | 130 | 155 | 180 | 8 | 175 | 116 | 38 | 75 |
| psilocybin | 5,284 | 4,983 | 186 | 601 | 259 | 808 | 89 | 138 | ||
| psilacetin | 337 | 1,178 | 108 | 335 | 395 | 9 | 210 | 350 | 112 | 157 |
| 4-HO-TMT | 720 | 2,267 | ||||||||
| aeruginascin | ||||||||||
| 4-AcO-TMT | 891 | |||||||||
| DOI | 607 | 713 | 11 | 5 | 41 | 2,254 | 1,857 |
Radioligands used, reference control compound used, and control Ki values for each 5-HT receptor were 5-HT1A = [3H]WAY100635 vs. 8-HO-DPAT (Ki = 0.6 nM), 5-HT1B = [3H]GR125743 vs. ergotamine tartrate (Ki = 4 nM), 5-HT1D = [3H]GR125743 vs. ergotamine tartrate (Ki = 4 nM), 5-ht1e = [3H]5-HT vs. 5-HT (Ki = 2 nM), 5-HT2A = [3H]ketanserin vs. clozapine (Ki = 4 nM), 5-HT2B = [3H]LSD vs. SB206553 (Ki = 18 nM), 5-HT2C = [3H]mesulergine vs. ritanserin (Ki = 1 nM), 5-HT5A = [3H]LSD vs. ergotamine tartrate (Ki = 12 nM), 5-HT6 = [3H]LSD vs. clozapine (Ki = 7 nM), 5-HT7a = [3H]LSD vs. clozapine (Ki = 20 nM). No value = <50% inhibition of radioligand binding in the 10 μM primary screening. DOI = (±)-2,5-dimethoxy-4-iodoamphetamine.