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Binding affinity values of endomorphin 1 analogues (± SD) determined by competitive displacement of [3H]DAMGO from whole SH-SY5Y cells. Kiμ values determined by 7 concentrations ranging from 10 pM to 1 μM performed in triplicate. Data is the mean ± S.E.M.
| Compound | Kiμ (nM) |
|---|---|
| 1 | 1.11 ± 0.79 |
| 2 | 2.15 ± 1.18 |
| 3 | 2.92 ± 0.12 |
| 4 | 3.02 ± 0.14 |
| 5 | 15.4 ± 7.20 |
| 7 | 115 ± 42.1 |
| 8 | 121 ± 52.1 |
| 10 | 151 ± 66.1 |
| 11 | 148 ± 67.2 |
| 12 | 266 ± 122 |
| 13 | 0.059 ± 0.01 |
| 14 | 0.081 ± 0.03 |
