Table 2.
Functional Activity Characterization Using [35S]GTPγS Assays in Opioid Transfected Cell Lines
| [35S]GTPγS functional assaya | ||||||
|---|---|---|---|---|---|---|
| mMOR | mKOR | mDOR | ||||
| compound | EC50 (nM) | Emax (%) | EC50 (nM) | Emax (%) | EC50 (nM) | Emax (%) |
| corynanthedine | 104.24 ± 4.59 | 74.13 ± 1.24 | no activity | no activity | no activity | no activity |
| mitraciliatine | 228 ± 9.6 | 47.5 ± 0.05 | 218 ± 6.4 | 98.7 ± 5 | no activity | |
| isopaynantheine | 191.8 ± 5.8 | 50 ± 5 | 282.2 ± 18 | 93.5 ± 5 | no activity | |
| corynoxine | 202.8 ± 4.4 | 136.4 ± 3.3 | no activity | no activity | no activity | |
| corynoxine B | no activity | no activity | no activity | |||
| DAMGOb | 3.4 ± 0.2 | 100 | - | - | - | - |
| U50,488Hb | - | - | 9.5 ± 1.8 | 100 | - | - |
| DPDPEb | - | - | - | - | 16.2 ± 5.1 | 100 |
a
Efficacy and potency data were obtained using agonist i [35S]GTPγS binding assay. Efficacy is represented as EC50 (nM) and percent maximal stimulation (Emax) relative to standard agonist DAMGO (MOR), DPDPE (DOR), or U50,488H (KOR) at 1000 nM. Results are presented as nM ± SEM from three independent experiments performed in triplicate. The dash (–) denotes not determined or not applicable. No activity = no agonism at 1000 nM drug concentration or no antagonism of 100 nM prototypic control agonist.
b
Literature values from Uprety et al. Elife. 2021 Feb 8;10:e56519.