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. Author manuscript; available in PMC: 2017 Aug 15.
Published in final edited form as: Bioorg Med Chem. 2016 Jun 15;24(16):3842–3848. doi: 10.1016/j.bmc.2016.06.029

Table 1. Inhibition of agonist-stimulated [35S]GTPγS binding in cloned human μ, δ, and κ opioid receptors.

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Compound Ke (nM)a μ/κ δ/κ
μ, DAMGO δ, DPDPE κ, U69,593
JDTic 25 ± 4 74 ± 2 0.02 ± 0.01 1,250 3,800
1 3.96 ± 1.1 281 ± 44 0.051 ± 0.01 77 5,510
2 14.5 ± 2.6 590 ± 130 0.43 ± 0.12 33 1,372
3a 45.4 ± 15 1140 ± 70 0.51 ± 0.08 89 2,235
3b 49.2 ± 14 >3000 0.18 ± 0.01 273 >16,700
4a 57.1 ± 15 690 ± 250 0.51 ± 0.14 112 1,353
4b 154 ± 56 2,510 ± 490 1.75 ± 0.65 88 1,434
5 3.93 ± 0.73 118 ± 27 0.12 ± 0.02 33 983
a

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

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