G Protein–coupled receptorome screening for amphetamine and PEA analogsa
Data represent Ki (nanomolar) values obtained from nonlinear regression using the Cheng-Prusoff equation when inhibition was >50%. The results for amphetamine (AMPH) were reported previously (Schindler et al., 2019).
| AMPH | AEPEA | MEPEA | DEPEA | |
|---|---|---|---|---|
| Serotonin | ||||
| 5-HT1A | 2625 | >10,000 | 1966 | 1588 |
| 5-HT2B | 971 | >10,000 | >10,000 | >10,000 |
| Norepinephrine | ||||
| α2A | 420 | >10,000 | >10,000 | >10,000 |
| α2B | 192 | 1362 | 411 | 1013 |
| α2C | 171 | 1404 | 1805 | 2320 |
| NET | 31 | >10,000 | >10,000 | 108 |
| Dopamine | ||||
| DAT | >10,000 | >10,000 | >10,000 | 124 |
| Sigma | ||||
| σ2 | >10,000 | >10,000 | 806 | 1352 |
| Histamine | ||||
| H1 | >10,000 | 2541 | 5800 | >10,000 |
↵ a Ki values for the following receptors were >10,000 nM for all four drugs tested: serotonin receptors 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6, 5-HT7, and SERT; norepinephrine receptors α1A, α1B, α1D, β1, β2, and β3; dopamine D1, D2, D3, D4, and D5; histamine receptors H2, H3, and H4; opioid receptors μ, κ, and δ; muscarinic receptors M1, M2, M3, M4, and M5; σ1 receptor; benzodiazepine and peripheral benzodiazepine receptors.