TABLE 3.
In vitro functional results from the [35S]GTPγS functional assay in transfected CHO cells expressing cloned hMORs
EC50 and Emax values in parentheses are 95% CIs (unless noted) from curve-fitting analyses of these data shown in Fig. 2.
| Compound | EC50 (95% CI) nM | Emax [%DAMGO] (95% CI) |
|---|---|---|
| Buprenorphine | 16.1 (6.53–39.6) | 42.8 (37.2–48.4) |
| DAMGO | 34.8 (24.9–48.6) | 103 (96.4–109) |
| Fentanyl | 27.8 (22.6–34.2) | 110 (106–115) |
| 7-Hydroxymitragynine | 43.4 (25.5–73.8) | 41.3 (37.1–45.6) |
| 53 (S.E.M.: 4)a | 77 (S.E.M.: 5)a | |
| 7.65 (S.E.M.: 0.884)b | 96.8 (S.E.M.: 1.8)b | |
| Mitragynine | Not determined in the present study | 3.46 ((−0.047 to 6.97) |
| 203 (S.E.M.: 13)a | 65 (S.E.M.: 2.8)a | |
| 320 (S.E.M.: 14.7)b | 44.1 (S.E.M.: 0.62)b | |
| Morphine | 125 (84.8–184) | 92.6 (85.8–99.4) |
| Nalbuphine | 5.87 (4.18–8.23) | 22.8 (21.1–24.6) |
| 9.0 (S.E.M.: 1.6)c | 16 (S.E.M.: 0.4)c | |
| 1.86 (SE: 0.1)d | 12d | |
| Naltrexone | Not determined in the present study | 4.69 (0.162–9.22) |
| SNC 80 | Not determined | 20.7 (S.E.M.: 3.01) at 10 μM |
| U69,593 | Not determined | 30.1 (S.E.M.: 2.88) at 10 μM |
a
[35S]GTPγS functional assay in transfected CHO cells stably expressing cloned mouse MORs (Váradi et al., 2016).
b
Homogeneous time-resolved fluorescence cAMP functional assay in transfected CHO cells stably expressing cloned hMORs (Obeng et al., 2020).
c
[35S]GTPγS functional assay in transfected CHO cells stably expressing cloned mouse MORs (Selley et al., 1998).
d
[35S]GTPγS functional assay in transfected C6 Glioma cells stably expressing cloned rat MORs (Emmerson et al., 1996).