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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)
  1. aValues are expressed as the mean ± SEM of at least three independent measurements
  2. bAntagonist potency (IC50) determined versus EC90 of U50,488H for KORs and EC50 of SNC-80 for DORs
  3. cDegree of antagonism (Imax) normalized to nor-BNI for KORs and 4b for DORs
  4. dAgonist efficacy expressed as percent stimulation