Binding (Ki) of KDN bivalent ligands and monovalent controls to coexpressed and singly expressed δ and κ opioid receptors Competition binding assay was conducted on intact whole cells using 0.1 nM [3H]natrindole or 2.0 nM [3H]nor-BNI as radioligand. Each assay was performed in duplicate, and the data shown here are representative of at least three independent experiments (means ± S.E.).
| Ligand | [3H]Naltrindole | [3H]nor-BNI | ||||
|---|---|---|---|---|---|---|
| CDK | MDK | DOR | CDK | MDK | DOR | |
| KDN15 | 3.42 ± 1.06 | 3.38 ± 1.44 | 1.92 ± 0.68 | 3.62 ± 1.41 | 2.51 ± 1.19 | 1.82 ± 0.62 |
| KDN20 | 1.02 ± 0.50 | 3.23 ± 1.37 | 2.45 ± 1.09 | 1.90 ± 0.98 | 2.62 ± 1.29 | 2.45 ± 1.19 |
| KDN21 | 0.06 ± 0.03 | 1.38 ± 0.57 | 3.37 ± 1.46 | 0.16 ± 0.06 | 4.67 ± 2.06 | 3.01 ± 1.42 |
| KDN22 | 2.34 ± 1.08 | 2.44 ± 1.21 | 1.23 ± 0.58 | 4.56 ± 2.04 | 2.45 ± 1.04 | 2.18 ± 1.17 |
| KDN23 | 1.58 ± 0.69 | 3.62 ± 1.18 | 7.40 ± 2.20 | 5.24 ± 2.61 | 2.34 ± 1.20 | 2.51 ± 1.36 |
| KDN24 | 2.04 ± 0.98 | 7.46 ± 2.57 | 2.06 ± 0.73 | 3.88 ± 1.84 | 2.04 ± 0.93 | 1.69 ± 0.73 |
| DN21 | 1.91 ± 0.84 | 3.29 ± 1.04 | 1.98 ± 0.52 | 137.7 ± 54.6 | 147.6 ± 59.8 | 203.7 ± 9.98 |
| KN21 | 197.8 ± 67.9 | 137.7 ± 55.8 | 190.1 ± 79.9 | 4.35 ± 1.74 | 2.45 ± 1.23 | 1.58 ± 0.83 |