Table 1.
GPI |
MVD |
Receptor binding |
Ki ratio |
|||
---|---|---|---|---|---|---|
Cpd | IC50 (nM) | IC50 (nM) | Kiμ (nM) | Kiδ (nM) | Kiκ (nM) | μ/δ/κ |
1 | 22.4 ± 3.7 | 114 ± 9 | 0.448 ± 0.079 | 43.5 ± 4.1 | 0.536 ± 0.043 | 1/97/1.2 |
8a | 521 ± 67 | 5820 ± 1040 | 300 ± 8 | 4110 ± 80 | 238 ± 41 | 1/14/0.8 |
8b | 590 ± 85 | 4750 ± 790 | 224 ± 13 | 7800 ± 280 | 162 ± 8 | 1/35/0.7 |
10 | 647 ± 77 | 610 ± 78 | 96.0 ± 5.9 | 6820 ± 670 | 1850 ± 160 | 1/71/19 |
Fentanyl | 3.45 ± 0.45b | 9.45 ± 4.05b | 5.9 ± 1.4c | 568 ± 159c | 298 ± 40c | 1/96/51 |
LENK | 246 ± 39 | 11.4 ± 1.1 | 9.43 ± 2.07 | 2.53 ± 0.35 | 4570 ± 550 | 1/0.3/485 |