Table 2. [3H]Diprenorphine displacement with 6′-GNTI and other opioid ligands.
Binding affinity | 6′GNTI | Diprenorphine | NorBNI | NTI |
---|---|---|---|---|
IC50, nM | ||||
KOP | 50.9 ± 9.8 | 1.09 ± 0.7 | 0.012 ± 0.02 | 26.6 ± 4.2 |
DOP | 4.7 ± 1.4 | 1.9 ± 2.3 | 81.2 ± 1.4 | 0.004 ± 0.006 |
MOP | 264.4 ± 66.7 | 0.5 ± 0.06 | 192.3 ± 37.8 | 34.6 ± 8.9 |
IC50H, nM | ||||
KOP/DOP | 7.7 ± 1.7 | 1.13 ± 0.2 | 0.34 ± 08 (569.8 ± 18.7)* | 0.46 ± 0.5 (112.2 ± 3.5)* |
KOP/MOP | 34.9 ± 10.1 | 0.97 ± 0.02 | 12.0 ± 2.8 (>1,000)* | 78.9 ± 22.2 |
DOP/MOP | 195.1 ± 48.2 | 0.99 ± 0.1 | 931.1 ± 79.5 | 37.4 ± 2.1 |
Data are mean ± SEM (n = 2-3). IC50H, high-affinity IC50.
Values in parentheses represent the low-affinity IC50 values.