Table 1.
Binding affinities and selectivities at MOP, DOP and KOP receptors
| |
K
i
(nM)
a
|
Selectivity ratios |
|||
|---|---|---|---|---|---|
| MOP | DOP | KOP | DOP/MOP | KOP/MOP | |
| Oxycodoneb |
43.6 ± 1.5 |
1,087 ± 246 |
2,658 ± 367 |
25 |
61 |
| 14-OMC |
35.3 ± 2.1 |
116 ± 15 |
454 ± 6 |
3 |
13 |
|
1
b
|
31.7 ± 2.1 |
498 ± 79 |
1,648 ± 201 |
16 |
52 |
|
2
b
|
2.44 ± 0.13 |
107 ± 5 |
364 ± 7 |
44 |
149 |
|
3
b
|
5.38 ± 0.42 |
197 ± 29 |
378 ± 155 |
37 |
70 |
|
4 |
1.61 ± 0.05 |
28.8 ± 2.3 |
105 ± 45 |
18 |
65 |
|
5 |
0.54 ± 0.04 |
30.3 ± 2.9 |
200 ± 40 |
56 |
370 |
| 6 | 7.39 ± 0.34 | 239 ± 40 | 194 ± 68 | 32 | 26 |
aMembranes from rat brain were used. bData from [30]. Values represent the mean ± SEM of at least three experiments each performed in duplicate.