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. Author manuscript; available in PMC: 2016 Oct 1.
Published in final edited form as: Bioorg Med Chem. 2015 Aug 25;23(19):6379–6388. doi: 10.1016/j.bmc.2015.08.025

Table 1.

Inhibition of Agonist-Stimulated [35S]GTPγS Binding by Compounds in Cloned Human μ, δ, and κ Opioid Receptors

graphic file with name nihms720817u2.jpg
Compd Ke (nM)a
X R1 R2 μ, DAMGO δ, DPDPE κ, U69,593 μ/κ δ/κ
nor-BNI — — — 26 29 0.05 520 580
JDTic — — — 25 ± 4 74 ± 2 0.02 1255 3800
3a — — — 8.9 442 0.024 370 18,400
3b — — — 14.8 249 0.01 1480 24,900
4a OH CH3 H 67.5 ± 10.4 927 ± 350 0.69 ± 0.21 98 1344
4b F CH3 H 38.0 ± 6.4 1480 ± 350 0.18 ± 0.04 211 8211
4c F CH3 CH3 11.3 ± 4.3 903 ± 200 0.033 ± 0.01 342 27,363
4d OH H H 12.3 ± 1.0 240 ± 73 0.10 ± 0.03 123 2400
4e H H H 3.96 ± 1.1 281 ± 44 0.051 ± 0.01 77 5500
4f F H H 3.55 ± 1.1 128 ± 36 0.023 ± 0.01 154 5600
a

Ke values are the mean ±SEM of at least three independent experiments performed in duplicate.