Table 1.
Binding affinities of salvinorin A analogues at opioid receptors using [125I]IOXY as radioligand.39, 40
| Ki ± SD, nM | Selectivity | ||||
|---|---|---|---|---|---|
| Compound | μ | δ | κ | μ/κ | δ/κ |
| 1aa | > 1,000b | 5790 ± 980 | 1.9 ± 0.2 | > 526 | 3050 |
| 1b | > 10,000 | > 10,000 | 280 ± 20 | > 35 | > 35 |
| 1ca | 12 ± 1 | 1170 ± 60 | 90 ± 2 | 0.13 | 12 |
| 3ac | 110 ± 1 | > 10,000 | 90 ± 7 | 1.2 | > 100 |
| 3bc | 110 ± 1 | > 10,000 | 70 ± 7 | 1.6 | > 100 |
| 3cc | 10 ± 1 | 1410 ± 80 | 740 ± 40 | 0.01 | 2 |
| 3d | 1640 ± 90 | > 10,000 | 230 ± 20 | 7 | > 43 |
| 3e | 30 ± 2 | 1140 ± 60 | 550 ± 30 | 0.05 | 2 |
| 3f | 70 ± 4 | 1860 ± 140 | 540 ± 40 | 0.12 | 3 |
| 3g | 7550 ± 970 | > 10,000 | 900 ± 50 | 8 | > 11 |
| 3h | > 10,000 | > 10,000 | 800 ± 50 | > 12 | > 12 |
| 3i | 260 ± 210 | > 10,000 | 570 ± 40 | 13 | 0.45 |
| 3j | > 10,000 | > 10,000 | 410 ± 40 | > 24 | > 24 |
| 3k | 180 ± 20 | > 10,000 | 5490 ± 640 | 0.03 | > 2 |
| 3l | 10 ± 1 | 580 ± 30 | 70 ± 2 | 0.14 | 8 |
| 3mc | 10 ± 2 | 1380 ± 130 | 260 ± 20 | 0.04 | 5 |
| 3n | 10 ± 1 | 690 ± 30 | 80 ± 3 | 0.16 | 9 |
| 3o | 1030 ± 80 | > 10,000 | 2010 ± 110 | 0.5 | > 5 |
| 7a | 4180 ± 310 | > 10,000 | 30 ± 2 | 13 | > 330 |
| 7b | 3.1 ± 0.4 | 810 ± 30 | 7430 ± 880 | 0.0004 | 0.11 |
| 8a | > 10,000 | > 10,000 | 260 ± 30 | > 38 | > 38 |
| 8b | > 10,000 | > 10,000 | 1400 ± 110 | > 7 | > 7 |
| 9a | 4370 ± 310 | 3990 ± 290 | 5.7 ± 0.4 | 767 | 700 |
| 9b | 290 ± 70 | 1930 ± 70 | 1410 ± 80 | 0.21 | 1.4 |