Table 5.
Opioid activities of fentanyl-based MOR/COX MTAs. Data from [23].
| Compound | Structure (Refer to Figure 7) |
Functional Tests (Inhibition of the Contractile Response Generated by Electrical Stimulation) |
||
|---|---|---|---|---|
| DOR (MVD 1) |
MOR (GPI/LM/MP 2) | |||
| R1 | R2 | Opioid Agonism, Inhibition of Contraction Height (% at 1 μM or IC50 in nM) |
||
| 6.4 | Me | H | 17.9% | 0.7% |
| 6.5 | PhCH2 | H | IC50 = 1266 ± 355 nM | IC50 = 5164 ± 2043 nM |
| 6.6 | PhCH2CH2 | H | 19.5% | 3.1% |
| 6.7 | Me | OMe | 2.8% | 0% |
| 6.8 | PhCH2 | OMe | 8.3% | 3% |
| 6.9 | PhCH2CH2 | OMe | 0% | 6% |
1 isolated mouse vas deferens (MVD), 2 longitudinal muscle/myenteric plexus (LM/MP) of the guinea pig ileum (GPI).