Table 3.
Binding Affinity of compounds (1–6) for Human Opioid (subtype δ, κ and μ) and Cannabinoid (subtype CB1 and CB2) Receptors.
| Compound a | Opioid Receptors (%) | Cannabinoid Receptors (%) | |||
|---|---|---|---|---|---|
| δ | κ | μ | CB1 | CB2 | |
| 1 | 62.2 | nab | na | na | na |
| 2 | na | 51.4 | na | ntc | nt |
| 3 | 52.5 | 48.0 | 67.1 | na | na |
| 4 | na | na | 59.1 | na | na |
| 5 | na | na | na | na | na |
| 6 | na | na | na | 62.6 | 43.1 |
| 7 | na | na | na | na | na |
| 8 | na | na | na | na | na |
| 9 | na | na | na | na | na |
| Naloxoned | 106.4 | 101.6 | 97.0 | nt | nt |
| CP 55,940e | nt | nt | nt | 104.3 | 102.6 |
a
All compounds were tested at the concentration of 10 μM.
b
Not active (< 40%).
c
Not tested.
d
For opioid receptor binding affinity assay, the opioid receptor antagonist naloxone was used as positive control.
e
For cannabinoid receptor binding affinity assay, the cannabinoid receptor agonist (CP 55,940) was used as positive control.