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. Author manuscript; available in PMC: 2023 Apr 30.
Published in final edited form as: J Med Chem. 2022 Mar 7;65(6):5095–5112. doi: 10.1021/acs.jmedchem.2c00087

Table 4.

Potencies and Efficacies at the KOR and DOR of Compounds 1, 14–16, 25, 26, 31, and 32

selectivity KOR [35S]GTPγS Binding DOR [35S]GTPγS Binding
compd κ/μ δ/μ EC50 (nM) % Emax of U50,488H EC50 (nM) % Emax of SNC80
NAPa 163 747 28.8 ± 14.4 45.5 ± 4.4 15.2 ± 15.2 10.2 ± 3.1
1 5 76 14.8 ± 0.99 43.4 ± 1.36 26.9 ± 3.23 50.9 ± 5.25
14 4 282 6.3 ± 0.85 67.2 ± 2.53 35.5 ± 8.71 23.1 ± 0.97
15 12 8 85.4 ± 6.29 63.3 ± 2.50 6.2 ± 0.83 66.8 ± 4.24
16 15 198 13.3 ± 0.59 49.3 ± 1.07 42.3 ± 6.03 31.2 ± 1.49
25 4 65 1.7 ± 0.24 50.6 ± 0.95 59.4 ± 6.71 48.6 ± 3.41
26 3 206 7.0 ± 0.31 67.4 ± 3.00 70.4 ± 38.51 43.6 ± 7.31
31 7 29 16.3 ± 1.73 47.8 ± 0.85 38.8 ± 5.83 58.5 ± 3.13
32 1 612 1.0 ± 0.44 90.8 ± 2.34 31.4 ± 4.89 47.8 ± 0.95
a

The in vitro data for NAP adopted from ref 31.