Table 2.
Binding affinities of compounds 3, 5, 9 a–d and 16 a,b towards the μ‐, κ‐ and δ‐OR subtypes.
|
| |||||
|---|---|---|---|---|---|
|
Compound |
K i (nM±SEM)[a] |
Selectivity[b] |
|||
|
μ |
κ |
δ |
μ/κ |
μ/δ |
|
|
β‐FNA (3)c |
0.4±0.05 |
0.9±0.05 |
7.7±2.4 |
2 |
20 |
|
3 |
1.5±0.21 |
10±2.3 |
26±7.4 |
6.7 |
17 |
|
5 c |
0.7±0.25 |
2.6±0.0 |
0.7±0.05 |
4 |
1 |
|
9 a |
2.3±0.26 |
19±1.9 |
30±2.8 |
8.3 |
13 |
|
9 b |
1.5±0.45 |
10±2.2 |
36±6.5 |
6.7 |
24 |
|
9 c |
1.3±0.30 |
10±2.6 |
28±3.0 |
7.7 |
22 |
|
9 d |
4.0±0.39 |
11±1.4 |
63±9.9 |
2.8 |
16 |
|
16 a |
4.9±1.5 |
18±5.7 |
54±9.1 |
3.7 |
11 |
|
16 b |
3.3±0.8 |
25±5.1 |
58±11 |
7.6 |
18 |
[a] Binding affinities are displayed as mean K i values ±SEM derived from three to 11 individual experiments each done in triplicate. [b] Subtype selectivity for μ‐OR expressed as ratio of K i values. [c] Binding affinities as reported by Derrick et al.34