Abilities of test compounds to displace (±)-[125I]DOI at wild-type and mutant h5-HT2A receptors
Data are represented as the mean (S.E.M.) of Ki values from non-linear regression fits of a single binding site model from at least three independent experiments.
Drug | Ki | ||||
|---|---|---|---|---|---|
| WT | S5.43(239)A | S5.46(242)A | |||
| nM | |||||
| 5-MeO-DMT | 7.54 (1.06) | 105 (19)* | 36.0 (1.9)* | ||
| 5-HT | 4.84 (0.20) | 53.2 (8.0)* | 20.2 (0.9)* | ||
| 5-MeO-T | 1.34 (0.22) | 4.17 (0.68)* | 2.70 (0.29) | ||
| Psilocin | 11.8 (1.2) | 58.0 (3.7)* | 23.1 (3.3) | ||
| 5-Me-T | 11.7 (0.6) | 10.9 (1.3) | 25.8 (3.9) | ||
| Tryptamine | 29.7 (4.4) | 50.2 (6.6) | 36.0 (6.0) | ||
| DMT | 75.1 (6.0) | 116 (12) | 135 (20) | ||
| 1-Me-5-HT | 70.0 (1.2) | 320 (37)* | 5.73 (0.83)* | ||
| 1-iPr-5-MeO-T | 494 (91) | 786 (85) | 24.1 (0.8)* | ||
| LSD | 0.40 (0.02) | 0.41 (0.08) | 1.66 (0.32)* | ||
| DOI | 0.64 (0.06) | 2.19 (0.26)* | 0.83 (0.11) | ||
| DOM | 5.91 (0.97) | 46.4 (5.9)* | 5.04 (0.55) | ||
| 2CI | 0.73 (0.06) | 1.20 (0.22) | 1.28 (1.28) | ||
| 2-Et-DOM | 91.1 (9.7) | 460 (92)* | 38.5 (4.1)* | ||
| 5-Et-DOM | 22.4 (1.2) | 32.2 (1.9) | 31.5 (5.0) | ||
| DOH | 245 (28) | 2246 (144)* | 294 (54) | ||
| 5-H-DOM | 169 (12) | 343 (41) | 164 (7) | ||
| 2CH | 377 (67) | 782 (19) | 440 (23) | ||
↵* P < 0.05 for values of Δ pKi from ANOVA with Bonferroni post tests comparing mutant and wild-type values