Functional properties of DiPOA in human opioid receptor GTPγ[35S] binding assays
EC50 and Emax values represent the mean ± S.E.M. of n independent determinations. Emax values were normalized to the signal in absence of agonist (0%) and in the presence of 10 μM DAMGO, 1 μM U69,593, and 60 nM nociceptin for the mu, kappa, and ORL-1 assays, respectively.
Compound | Mu | Kappa | ORL-1 | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| EC50 | Emax | n | EC50 | Emax | n | EC50 | Emax | n | |||||||
| nM | % | nM | % | nM | % | ||||||||||
| DiPOA | 32.7 ± 8.1 | 85.1 ± 0.7 | 3 | 554 ± 100 | 67.0 ± 4.0 | 3 | 2940 ± 1229 | 72.9 ± 8.3 | 5 | ||||||
| Morphine | 119 ± 23 | 55.9 ± 3.5 | 3 | 350 ± 112 | 96.7 ± 5.7 | 3 | ND | ||||||||
| Naltrexone | Inactive | 2 | ND | ND | |||||||||||
| DAMGO | 202 ± 52 | 95.4 ± 0.5 | 8 | ND | ND | ||||||||||
| U69,593 | ND | 27.3 ± 12.9 | 96.3 ± 1.7 | 3 | ND | ||||||||||
| Nociceptin | ND |
| ND |
| 0.09 ± 0.06 | 98 ± 0.6 | 3 | ||||||||
ND, not determined.