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. Author manuscript; available in PMC: 2019 Aug 13.
Published in final edited form as: J Med Chem. 2018 Aug 29;61(17):7525–7545. doi: 10.1021/acs.jmedchem.8b00673

Table 4.

Inhibition of Agonist-Stimulated [35S]GTPγS Binding in Cloned Human μ, δ, and κ Opioid Receptors, Effects of Adding a 3,4-Double Bond

graphic file with name nihms-1043744-t0019.jpg
compd R1 R2 Ke (nM)a
 μ/κ δ/κ
μ, DAMGO δ, DPDPE κ, U69,593
27 H H 37.7 ± 7.9 >3000 1.07 ± 0.11 35 >2804
28 CH3 H 11.8 ± 1.2 >3000 0.88 ± 0.18 13.4 >3410
29 H CH3 28.9 ± 3.7 >3000 9.43 ± 2.9 3 >318
30 CH3 CH3 1.09 ± 0.11 1930 ± 330 1.81 ± 0.27 0.6 1066
a

Data are mean ± SEM of at least three independent experiments conducted in duplicate. None of the compounds had agonist activity at 10 μM.