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Activation Profile of Opioid ligands in HEK-δ Cells |
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| LIGAND |
IC50 ± SEM (nM) |
Max Inhibition % |
|
|
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| Butorphanol |
61 ± 12 |
64 ± 4$ |
| Cyclazocine |
6 ± 3 |
53 ± 2** |
| Dezocine |
477 ± 152 |
39 + 8 |
| Etorphine |
0.2 ± 0.1 |
67 ± 3$$ |
| Fentanyl |
2039 ± 554 |
71 ± 7$$ # |
| Hydromorphone |
54 ± 31 |
65 ± 5$ |
| Lofentanil |
0.8 ± 0.4 |
62 ± 7$ |
| Metazocine |
159 ± 70 |
77 ± 4$$ |
| Met-enkephalin |
22 ± 17 |
49 ± 6## |
| Morphine |
1101 ± 614 |
39 ± 4** |
| Nalbuphine |
545 ± 378 |
55 ± 7* |
| Nalorphine |
Antagonist |
|
| Naltrexone |
Antagonist |
|
| SKF 10047 |
184 ± 121 |
68 ± 9$$ |
| WIN 44,441 |
40 ± 25 |
54 ± 6* |
| Xorphanol |
8 ± 2 |
76 ± 4$$ ## |
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Inhibitory effect of opioid ligands on Forskolin-stimulated Adenylyl Cyclase activity was measured as described under Materials and Methods. Data for IC50's represent the mean ± SEM obtained from two or more experiments carried out in duplicate. Maximum inhibition is the mean ± SEM of maximum inhibition obtained from a best fit curve as described under "Materials and Methods" (** = P < 0.001, * = P < 0.05 compared to Metazocine), ($$ = P < 0.001, $ = P < 0.05 compared to morphine), (## = P < 0.001, # = P < 0.05 compared to met-enkephalin). | ||
Gharagozlou et al. BMC Neuroscience 2002 3:19 doi:10.1186/1471-2202-3-19 |
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