Table 2.
Agonist activities at the MOP receptor
| |
[
35
S]GTPγS functional assay
a
|
Calcium mobilization assay
b
|
||
|---|---|---|---|---|
| EC 50 (nM) | E max (%) c | EC 50 (nM) | E max (%) c | |
| Oxycodone |
500 ± 128 |
92 ± 9 |
1,176 ± 347 |
38 ± 3 |
| 14-OMC |
325 ± 94 |
137 ± 55 |
973 ± 204 |
72 ± 7 |
|
1 |
273 ± 24 |
98 ± 4 |
957 ± 233 |
57 ± 4 |
|
2 |
42.5 ± 14.9 |
97 ± 15 |
116 ± 9 |
69 ± 7 |
|
3 |
26.2 ± 1.7 |
85 ± 3 |
140 ± 21 |
61 ± 6 |
|
4 |
25.6 ± 9.5 |
107 ± 26 |
56.1 ± 11.3 |
59 ± 8 |
|
5 |
1.64 ± 0.19 |
133 ± 7 |
21.7 ± 5.5 |
70 ± 8 |
|
6 |
25.1 ± 3.6 |
121 ± 27 |
173 ± 21 |
84 ± 10 |
| DAMGO | 20.2 ± 5.6 | 100 | 42.7 ± 7.6 | 100 |
aMembranes from CHO cells stably transfected with human MOP receptors were used. bCHO cells co-expressing Gαqi5 protein and recombinant human MOP receptor were used. cEmax is expressed in percentage relative to maximal DAMGO induced stimulation in each assay (225 ± 32% and 217 ± 21% in [35S]GTPγS functional and calcium mobilization assay, respectively, set as 100%). Values represent the mean ± SEM of at least three experiments each performed in duplicate or triplicate.