Table 1.
Summary of antagonist affinity and selectivity for κ-, μ- and δ-receptors in the competitive [3H]-diprenorphine binding assay.
| Ligand | Competitive binding with [3H]-diprenorphine Ki (nM;±SEM) |
κ-selectivity |
|||
|---|---|---|---|---|---|
| κ | μ | δ | vs. μ | vs. δ | |
| NorBNI | 0.29 ± 0.02 | 3.99 ± 2.38 | 0.46 ± 0.09 | 14 | ~2 |
| GNTI | 0.67 ± 0.18 | 9.04 ± 1.99 | 2.86 ± 1.45 | ~14 | ~4 |
| 5’-AMN | 1.36 ± 0.98 | 7.50 ± 6.45 | 1.34 ± 2.12 | ~6 | 1 |
| 5’-MABN | 0.27 ± 0.08 | 0.88 ± 0.51 | 1.35 ± 1.56 | ~3 | 5 |
Ki values for the test ligands were determined by competitive displacement of [3H]-diprenorphine binding in CHO-κ, C6-μ and C6-δ cell membranes. Values are the mean ± SEM of n = 2 in triplicate experiments.