Stimulation of [35S]GTPγS binding by BU08028, compared with buprenorphine, morphine, and other prototypical agonists at NOP and opioid receptors
Data show mean ± S.D. for at least two experiments conducted in triplicate. SR16435 data are from Khroyan et al., 2007.
| NOP | μ | δ | κ | |||||
|---|---|---|---|---|---|---|---|---|
| EC50 | %Stimulated | EC50 (nM) | %Stimulated | EC50 | %Stimulated | EC50 | %Stimulated | |
| nM | nM | nM | nM | |||||
| Buprenorphine | 251 ± 94 | 15.5 ± 5.8 | 10.2 ± 2.2 | 28.7 ± 1.0 | >10,000 | >10,000 | ||
| N/OFQ | 8.11 ± 1.4 | 100 | ||||||
| DAMGO | 35.3 ± 0.5 | 100 | ||||||
| DPDPE | 6.90 ± 0.4 | 100 | ||||||
| U69593 | 78.5 ± 8.8 | 100 | ||||||
| SR16435 | 28.7 ± 0.6 | 45.0 ± 5.1 | 2.73 ± 0.01 | 29.5 ± 10 | N.D. | >10,000 | ||
| BU08028 | 78.6 ± 49 | 48 ± 13 | 6.03 ± 2.1 | 21.1 ± 8.7 | —* | 10.8 ± 6.8 | >10,000 | |
N.D., not determined.
↵* Stimulation was too low to accurately determine EC50 value.