Table 2. Binding affinities of compounds (9a–f) a .
| Compound | MOR | KOR | DOR | M/K | M/D | 
| K
i (nM) | |||||
| 9a | 7.02 ± 0.77 | >100 | 173.4 ± 43.6 | >14.2 | 24.7 | 
| 9b | 6.91 ± 0.88 | >100 | 103.7 ± 17.0 | >14.5 | 15.0 | 
| 9c | 2.00 ± 0.17 | 77.9 ± 31 | 65 ± 19.0 | 39.0 | 32.5 | 
| 9d | 1.25 ± 0.23 | 18.97 ± 5.3 | 34.4 ± 5.00 | 15.2 | 27.5 | 
| 9e | 3.73 ± 0.14 | >100 | 198.4 ± 69 | >26.8 | 53.2 | 
| 9f | 3.29 ± 0.36 | 119 ± 50.4 | 130.3 ± 37 | 36.2 | 39.6 | 
| 9g | 40.59 ± 3.65 | >100 | 423.9 ± 88 | >2.5 | 10.4 | 
| 1 b | 0.37 ± 0.07 | 277.51 ± 7.97 | 60.72 ± 5.58 | 747 | 163 | 
| 2 c | 0.10 ± 0.02 | 2.90 ± 0.66 | 10.26 ± 6.76 | 29.0 | 102.6 | 
| Morphine | 4.60 ± 1.81 | ||||
a[125I]BNtxA (0.1 nM) competition binding assays were performed in membranes prepared from CHO cells expressing mouse MOR, DOR, or KOR, as previously described. Protein concentrations were between 10–20 μg mL–1 and the incubation time was 90 minutes.19Ki was determined by nonlinear regression analysis (GraphPad Prism). Assays were performed at least 3 times and means ± SEM are reported.
bValues are taken from ref. 12.
cValues are taken from ref. 13.