|
Activation Profiles of Opioid ligands in HEK-μ Cells |
||
| Agonist |
IC50 ± SEM (nM) |
Max Inhibition (%) |
|
|
||
| β-Endorphin |
526 ± 105 |
71 ± 5 |
| Butorphanol |
3 ± 2 |
58 ± 5 |
| Cyclazocine |
21 ± 8 |
37 ± 2**## |
| DAMGO |
35 ± 9 |
58 ± 5 |
| Dezocine |
1.3 ± 0.6 |
43 ± 2**## |
| Etorphine |
0.6 ± 0.3 |
60 ± 6 |
| Fentanyl |
8.4 ± 1.6 |
69 ± 4⊕ |
| Hydromorphone |
0.8 ± 0.1 |
67 ± 4⊕ |
| Lofentanil |
3.8 ± 2.0 |
56 ± 6 |
| Metazocine |
2.0 ± 0.1 |
41 ± 4**## |
| Morphine |
17 ± 8 |
48 ± 4*## |
| Nalbuphine |
11 ± 2 |
49 ± 4*## |
| Nalorphine |
2.7 ± 1.4 |
50 ± 2# |
| Xorphanol |
3.4 ± 1.7 |
29 ± 2** ⊕⊕## |
| Naltrexone |
Antagonist |
|
| SKF 10047 |
Antagonist |
|
| WIN 44,441 |
Antagonist |
|
|
Inhibitory effect of opioid ligands on Forskolin-stimulated adenylyl cyclase activity was measured as described under "Materials and Methods". Data for IC50's represent the mean ± SEM obtained from two or more experiments carried out in duplicate. Maximum inhibition data represent the mean ± SEM obtained from the best fit curve for data from three to four experiments carried out in duplicate. (** = P < 0.001, * = P < 0.05; compared to fentanyl), (⊕⊕ = P < 0.001, P, ⊕ = P < 0.05 compared to morphine), (## = P < 0.001, # = P < 0.05; compared to β-endorphin). | ||
Gharagozlou et al. BMC Pharmacology 2003 3:1 doi:10.1186/1471-2210-3-1 |
||