Table 3 Evaluation of functional activity at KORs and DORs using Eurofins DiscoverX HitHunter® cAMP Assay
From: Design, synthesis, and preliminary evaluation of a potential synthetic opioid rescue agent
Cmpd | KOR antagonism IC50 (nM)a,b (Imax)c | KOR agonism EC50 (nM)a (% efficacy)d | DOR antagonism IC50 (nM)a,b (Imax)c | DOR agonism EC50 (nM)a (% efficacy)d |
|---|---|---|---|---|
4b | 5.53 ± 1.02 (41.31 ± 6.83) | 0.64 ± 0.32 (56.46 ± 7.15) | 177.16 ± 48.90 (99.57 ± 1.93) | > 10,000 |
14 | 8.15 ± 1.10 (49.27 ± 11.54) | 1.56 ± 0.69 (58.71 ± 5.77) | > 10,000 | 2.09 ± 0.80 (47.42 ± 2.58) |
20 | 8.70 ± 1.89 (46.68 ± 2.95) | 0.67 ± 0.39 (39.11 ± 4.70) | 4.06 ± 2.36 (29.48 ± 5.94) | 1.04 ± 0.35 (48.05 ± 1.87) |
21 | 10.68 ± 4.48 (62.72 ± 18.41) | 0.12 ± 0.03 (41.17 ± 8.81) | > 10,000 | 2.28 ± 0.72 (45.47 ± 2.38) |
22 | 33.74 ± 3.77 (84.97 ± 6.39) | > 10,000 | 368.31 ± 136.17 (89.22 ± 4.30) | > 10,000 |
28 | 8.54 ± 3.54 (47.32 ± 12.19) | 0.14 ± 0.04 (44.09 ± 8.43) | > 10,000 | 0.72 ± 0.22 (48.92 ± 3.66) |
29 | 4.49 ± 2.02 (46.84 ± 16.34) | 0.43 ± 0.18 (59.08 ± 8.54) | > 10,000 | 0.19 ± 0.09 (54.96 ± 3.44) |
30 | 8.75 ± 2.05 (89.12 ± 0.69) | > 10,000 | 48.58 ± 24.06 (49.76 ± 1.50) | 0.86 ± 0.33 (32.98 ± 3.21) |
nor-BNI | 2.10 ± 0.64 (98.54 ± 2.47) | NT | NT | NT |
Salvinorin A | NT | 0.026 ± 0.005 (98.66 ± 0.85) | NT | NT |
U50488H |  | 0.18 ± 0.06 (98.99 ± 0.83) |  |  |
Naltrindole | NT | NT | 0.51 ± 0.17 (100.14 ± 6.20) | NT |
SNC-80 | NT | NT | NT | 1.27 ± 0.22 (76.33 ± 1.38) |