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. 2014 Feb 27;57(6):2237–2246. doi: 10.1021/jm400879w

Table 2. Opioid Receptor Binding Determined by Radioligand Displacement in Membrane Preparations with hMOR, hDOR, and hKOR Receptors Expressed in CHO Cells45,46.

helix series 1
∼B∼B∼
2
∼A∼B∼
3
∼B∼A∼
4
∼A∼A∼
5
∼A∼G∼
6
∼G∼A∼
7
∼G∼G∼
μ-Binding (Ki’s in nM) vs [3H]DAMGO
L 21 ± 0.90 8.2 ± 0.60 13 ± 0.54 11 ± 1.4 9.6 ± 0.18 9.8 ± 0.97 5.0 ± 0.37 S**
G 9.1 ± 0.39 2.6 ± 0.29 6.1 ± 0.31 6.2 ± 0.47 2.2 ± 0.30 2.9 ± 0.32 3.5 ± 0.55 S*
U 29 ± 3.1 29 ± 0.67 21 ± 2.6 14 ± 2.3 13 ± 0.97 13 ± 1.2 12 ± 1.8 S
δ-Binding (Ki’s in nM) vs [3H]naltrindole
L 35 ± 3.0 12 ± 0.94 19 ± 0.67 12 ± 0.99 12 ± 1.0 8.2 ± 0.29 7.0 ± 0.57 S**
G 11 ± 1.2 3.6 ± 0.23 14 ± 2.1 7.9 ± 1.0 6.3 ± 0.094 5.7 ± 0.35 7.1 ± 1.0 S*
U 23 ± 2.8 15 ± 0.79 25 ± 1.6 16 ± 1.9 15 ± 0.98 11 ± 0.91 13 ± 2.2 S
κ-Binding (Ki’s in nM) vs [3H]U69,593
L 17 ± 1.9 5.7 ± 0.13 17 ± 1.6 15 ± 0.39 13 ± 0.76 23 ± 2.3 8.4 ± 1.2 S**
G 6.9 ± 0.58 2.3 ± 0.31 12 ± 0.94 8.9 ± 1.0 6.3 ± 0.41 11 ± 0.26 4.4 ± 0.47 S*
U 14 ± 1.4 16 ± 0.16 26 ± 1.6 14 ± 2.1 15 ± 1.3 20 ± 1.4 15 ± 1.9 S