Stimulation of [35S]GTPγS binding to membranes from SH-SY5Y cells by buprenorphine and analogs
| EC50 | Maximal Effect4-a | |
|---|---|---|
| nM | % | |
| BU46 | 0.21 ± 0.04 | 49.4 ± 1.5 |
| BU47 | 0.40 ± 0.07 | 51.0 ± 1.6 |
| BU61 | 0.23 ± 0.04 | 45.8 ± 1.6 |
| BU95 | 0.33 ± 0.06 | 53.8 ± 0.7 |
| BU96 | 0.56 ± 0.08 | 51.7 ± 0.8 |
| Buprenorphine | 0.18 ± 0.10 | 73.4 ± 2.1 |
Membranes from SH-SY5Y cells were incubated with [35S]GTPγS (80 pM), GDP (3 μM), and varying concentrations of opioid for 60 min at 30°C as described in Materials and Methods. Data represent means ± S.E. from at least three determinations each performed in triplicate.
↵4-a Percentage of response caused by a maximal (3 μM) concentration of fentanyl.