Compound | R2 | R3 | R4 | R6 | EC50 | Emax | n |
---|---|---|---|---|---|---|---|
nM | % | ||||||
β-PEA | H | H | H | H | 106 ± 5 | 99.9 ± 0.05 | 32 |
2-Fluoro-β-PEA | F | H | H | H | 51.6 ± 6.2 | 97.3 ± 4.8 | 4 |
3-Fluoro-β-PEA | H | F | H | H | 115 ± 24 | 109 ± 5 | 6 |
4-Fluoro-β-PEA | H | H | F | H | 425 ± 3 | 84.4 ± 7.2 | 3 |
2-Chloro-β-PEA | Cl | H | H | H | 30.0 ± 3.5 | 90.4 ± 4.3 | 9 |
3-Chloro-β-PEA | H | Cl | H | H | 116 ± 16 | 84.6 ± 3.4 | 11 |
4-Chloro-β-PEA | H | H | Cl | H | 830 ± 49 | 75.5 ± 2.3 | 9 |
2,6-Dichloro-β-PEA | Cl | H | H | Cl | 45.6 ± 2.7 | 76.9 ± 1.6 | 29 |
2-Bromo-β-PEA | Br | H | H | H | 83.1 ± 17.4 | 92.8 ± 3.4 | 6 |
3-Bromo-β-PEA | H | Br | H | H | 278 ± 48 | 84.9 ± 3.2 | 6 |
4-Bromo-β-PEA | H | H | Br | H | 1770 ± 140 | 93.8 ± 3.7 | 3 |
2-Methyl-β-PEA | Me | H | H | H | 157 ± 26 | 96.1 ± 6.8 | 6 |
3-Methyl-β-PEA | H | Me | H | H | 475.0 ± 68 | 79.6 ± 8.6 | 3 |
4-Methyl-β-PEA | H | H | Me | H | 1810 ± 160 | 95.4 ± 7.9 | 4 |
2,6-Dimethyl-β-PEA | Me | H | H | Me | 307 ± 31 | 74.0 ± 4.5 | 3 |
2-Hydroxy-β-PEA | OH | H | H | H | 645 ± 40.4 | 86.5 ± 7.9 | 3 |
3-Hydroxy-β-PEA | H | OH | H | H | 2080 ± 390 | 85.7 ± 4.1 | 6 |
4-Hydroxy-β-PEA | H | H | OH | H | 425 ± 22 | 88.6 ± 2.2 | 27 |
2-Methoxy-β-PEA | MeO | H | H | H | 143 ± 20 | 85.1 ± 9.7 | 3 |
3-Methoxy-β-PEA | H | MeO | H | H | 741 ± 70 | 76.0 ± 7.2 | 3 |
4-Methoxy-β-PEA | H | H | MeO | H | 2070 ± 290 | 105 ± 7 | 3 |