Skip to main content
. 2022 Nov 2;5(11):1181–1196. doi: 10.1021/acsptsci.2c00177

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
a

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.