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∼ |
S° |
---|---|---|---|---|---|---|---|---|
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 |