TABLE 2

Affinities and potencies of substituted tryptamines for hSERT

DrugHEK-hSERTHEK-hSERTHEK-hSERT
Inhibition of [125I]RTI-55 BindingInhibition of [3H]5-HT UptakeRatio [125I]RTI-55 Binding/ [3H]5-HT Uptake
Ki nM ± S.E.M. (n)IC50 nM ± S.E.M. (n)
DMT4560 ± 350 (21)712 ± 99 (22)6.40
DET1200 ± 170 (3)a254 ± 29 (4)b4.72
DPT480 ± 34 (4)c172 ± 35 (5)c2.79
4-OH-DET1411 ± 99 (3)d383 ± 41 (4)3.68
4-OH-DiPT419 ± 37 (3)c163 ± 52 (4)a2.57
4-OH-DMT3650 ± 270 (3)1140 ± 210 (3)3.20
4-OH-MET2310 ± 130 (3)830 ± 170 (3)2.78
4-OH-MIPT483 ± 20 (4)c373 ± 16 (3)1.29
4-OH-MPT1180 ± 240 (4)c575 ± 72 (4)2.05
4-AcO-DET13100 ± 2600 (5)a2600 ± 900 (3)c5.04
4-AcO-DIPT1180 ± 100 (3)a237 ± 77 (4)a4.98
4-AcO-DMT8000 ± 1200 (3)8300 ± 1300 (3)c0.96
4-AcO-MET17,500 ± 1800 (4)c3240 ± 310 (6)c5.40
4-AcO-MiPT10,400 ± 1200 (4)b5800 ± 1200 (5)c1.79
4-MeO-DiPT12.1 ± 3.1 (5)c11.1 ± 2.7 (4)c1.09
4-MeO-MiPT38.0 ± 3.8 (3)c53 ± 13 (3)c0.72
5-MeO-DALT1270 ± 89 (4)a930 ± 110 (4)1.37
5-MeO-DBT1180 ± 2402120 ± 190 (4)c0.56
5-MeO-DiPT874 ± 71 (3)c239 ± 39 (3)b3.66
5-MeO-DPT1070 ± 260 (3)c910 ± 190 (4)1.18
5-MeO-MiPT4040 ± 500 (3)2680 ± 460 (3)c1.51
5-Cl-DMT830 ± 140 (3)c394 ± 66 (5)2.11
Standards
Cocaine590 ± 50 (38)c349 ± 30 (25)a1.69
METH124,600 ± 1400c59,500 ± 1300 (4)c2.09
LSD>100,000 (11)c>100,000 (10)c1
DOM48,500 ± 3400 (7)c53,100 ± 8000 (9)c0.91
MDMA14700 ± 2900 (3)e109 ± 17 (5)e135

  • (n), number of experiments conducted in duplicate.

  • aP < 0.001, one-way ANOVA followed by Dunnett’s multiple comparison test compared with DMT.

  • bP < 0.05, one-way ANOVA followed by Dunnett’s multiple comparison test compared with DMT.

  • cP < 0.0001, one-way ANOVA followed by Dunnett’s multiple comparison test compared with DMT.

  • dP < 0.01, one-way ANOVA followed by Dunnett’s multiple comparison test compared with DMT.

  • eData from Eshleman et al. (2017).