Table 1. Receptor Interaction Profiles for LSD and Other Classic Serotonergic Hallucinogens at Human Receptors.
| LSDa | Psilocinb | DMTb | Mescalinea | ||
|---|---|---|---|---|---|
| 5-HT1A | Receptor binding Ki±SD (μM) | 0.003±0.0005 | 0.123±0.02 | 0.075±0.02 | 4.6±0.4 |
| 5-HT2A | Receptor binding Ki±SD (μM) | 0.004±0.001 | 0.049±0.01 | 0.237±0.04 | 6.3±1.8 |
| 5-HT2A | Activation potency EC50±SD (μM) | 0.261±0.15 | 0.721±0.55 | 0.076±0.03 | 10±1.8 |
| 5-HT2A | Activation efficacy % maximum±SD | 28±10 | 16±8 | 40±11 | 56±15 |
| 5-HT2B | Activation potency EC50±SD (μM) | 12±0.4 | >20 | 3.4±3.2 | >20 |
| 5-HT2B | Activation efficacy % maximum±SD | 71±31 | 19±6 | ||
| 5-HT2C | Receptor binding Ki±SD (μM) | 0.015±0.003 | 0.094±0.009 | 0.424±0.15 | 17±2.0 |
| α2A | Receptor binding Ki±SD (μM) | 0.67±0.18 | 6.7±1.1 | 1.3±0.2 | >15 |
| α1A | Receptor binding Ki±SD (μM) | 0.012±0.002 | 2.1±0.01 | 2.1±0.4 | 1.4±0.2 |
| D1 | Receptor binding Ki±SD (μM) | 0.31±0.09 | >14 | 6.0±0.9 | >14 |
| D2 | Receptor binding Ki±SD (μM) | 0.025±0.0004 | 3.7±0.6 | 3.0±0.4 | >10 |
| D3 | Receptor binding Ki±SD (μM) | 0.10±0.01 | 8.9±0.8 | 6.3±2.1 | >17 |
| H1 | Receptor binding Ki±SD (μM) | 1.1±0.2 | 1.6±0.2 | 0.22±0.03 | >25 |
| TAAR1c | Activation potency EC50±SD (μM) | >20 | >30 | >10 | >10 |
| NET | Receptor binding Ki±SD (μM) | >30 | 13±1.7 | 6.5±1.3 | >30 |
| NET | Inhibition potency IC50 (μM) (95% CI) | >100 | 14 (10–19) | 3.9 (2.8–5.3) | >100 |
| DAT | Receptor binding Ki±SD (μM) | >30 | >30 | 22±3.9 | >30 |
| DAT | Inhibition potency IC50 (μM) (95% CI) | >100 | >100 | 52 (37–72) | >100 |
| SERT | Receptor binding Ki±SD (μM) | >30 | 6.0±0.3 | 6.0±0.6 | >30 |
| SERT | Inhibition potency IC50 (μM) (95% CI) | >100 | 3.9 (3.1–4.8) | 3.1 (2.4–4.0) | >100 |
| Dosed | Mg | 0.1 | 12 | 40 | 300 |
Abbreviations: DAT, dopamine transporter; NET, norepinephrine transporter; SERT, serotonin transporter.
All data were generated using the same assays across substances to allow for direct comparisons.
d
Estimated average psychoactive dose in humans from Passie et al, 2008 and Nichols, 2004.