Raynor K, Kong H, Chen Y, Yasuda K, Yu L, Bell GI, Reisine T
Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid
receptors. Mol Pharmacol 45 : 330-334 (1994)
| Ligand | Ki, nm | ||
|---|---|---|---|
| Delta Receptor [3H]naltrindole |
Kappa Receptor [3H]U-69,593 |
Mu Receptor [3H]DAMGO | |
| Delta-selective Agonists | |||
| Leu-enkephalin | 4.0 | >1000 | 3.4 |
| Met-enkephalin | 1.7 | >1000 | 0.65 |
| Deltorphin II | 3.3 | >1000 | >1000 |
| DADLE | 0.74 | >1000 | 16 |
| DPDPE | 14 | >1000 | >1000 |
| DSLET | 4.8 | >1000 | 39 |
| BW373U86 | 0.013 | 17 | 26 |
| SIOM | 1.7 | >1000 | 33 |
| Delta-selective Antagonists | |||
| BNTX | 0.66 | 55 | 18 |
| NTB | 0.013 | 13 | 12 |
| Naltrindole | 0.02 | 66 | 64 |
| Kappa-selective Agonists | |||
| Dynorphin A | >1000 | 0.5 | 32 |
| (+)Bremazocine | 2.3 | 0.089 | 0.75 |
| EKC | 101 | 0.40 | 3.1 |
| U-50,488 | >1000 | 0.12 | >1000 |
| Spiradoline | >1000 | 0.036 | 21 |
| U-69,593 | >1000 | 0.59 | >1000 |
| Kappa-selective Antagonists | |||
| Nor-BNI | 65 | 0.027 | 2.2 |
| Mu-selective Agonists | |||
| Beta-endorphin | 1.0 | 52 | 1.0 |
| Dermorphin | >1000 | >1000 | 0.33 |
| DAMGO | >1000 | >1000 | 2.0 |
| PL017 | >1000 | >1000 | 30 |
| Fentanyl | >1000 | 255 | 0.39 |
| Morphine | >1000 | 538 | 14 |
| Sufentanyl | 50 | 75 | 0.15 |
| Mu-selective Antagonists | |||
| CTOP | >1000 | >1000 | 0.18 |
| Beta-FNA * | 48 | 2.8 | 0.33 |
| Naloxonazine | 8.6 | 11 | 0.054 |
| Non-selective Agonists | |||
| Etorphine | 1.4 | 0.13 | 0.23 |
| Levorphanol | 5.0 | 6.5 | 0.086 |
| Methadone | >1000 | >1000 | 0.72 |
| Non-selective Antagonists | |||
| Diprenorphine | 0.23 | 0.017 | 0.072 |
| (-)-Naloxone | 17 | 2.3 | 0.93 |
| Naltrexone | 149 | 3.9 | 1.0 |
| Beta-CNA * | 115 | 0.083 | 0.90 |
| Mixed Agonists/Antagonists | |||
| Nalbuphine | >1000 | 3.9 | 11 |
| Nalorphine | 148 | 1.1 | 0.97 |