Table 1.
Brief summary of functional profiles of compounds with selective MOP agonist or mixed NOP/MOP agonist actions in NHPs.
| Binding Ki NOP/MOP | Intrinsic activity | Analgesia | Itch (pruritus) | Respiratory depression | Tolerance | Physical dependence | Abuse liability | ||
|---|---|---|---|---|---|---|---|---|---|
| MOP | NOP | ||||||||
| Morphine | < 0.001 | 0.83 | − | + | + | + | + | + | + |
| Fentanyl | < 0.001 | 0.97 | − | + | + | + | N.D. | N.D. | + |
| Cebranopadol | 0.78 | 1 | 0.89 | + | − | − | N.D. | N.D. | + |
| AT-121 | 4.49 | 0.14 | 0.41 | + | − | − | − | − | − |
| BU08028 | 0.25 | 0.21 | 0.48 | + | − | − | N.D. | − | − |
| BU10038 | 0.06 | 0.18 | 0.34 | + | − | − | − | − | − |
N.D.: not determined
+:
detected
−:
not detected.
The data of binding affinity and intrinsic activity are based on the studies by Ding et al. 2016; Emmerson et al. 1996; Khroyan et al. 2011; Kiguchi et al. 2019; Linz et al. 2014. The in vivo functional data in NHPs are based on the studies by Ding et al. 2016; Ding et al. 2018; Kiguchi et al. 2019; Sukhtankar et al. 2014b.