Competition of 125I-[Tyr10]OFQ/N(1–11) binding in mouse brain membranes
| Drug | 125I-[Tyr14]OFQ | 125I-[Tyr10]OFQ/N(1–11) | Ratio | ||
|---|---|---|---|---|---|
| Ki | Hill Slope | Ki | Hill Slope | ||
| nM | nM | ||||
| OFQ/N and related peptides | |||||
| OFQ/N | 0.17 ± 0.06 | 0.60 | 0.007 ± 0.002 | 0.73 | 24 |
| [Tyr14]OFQ/N | 0.65 ± 0.36 | 0.43 | 0.007 ± 0.0003 | 1.1 | 93 |
| Iodo[Tyr14]OFQ/N | 0.12 ± 0.03 | 0.93 | 0.006 ± 0.002 | 0.78 | 20 |
| OFQ/N (1–11) | 262 ± 80 | 0.67 | 8.7 ± 1.9 | 0.73 | 30 |
| [Tyr10]OFQ/N (1–11) | 79.8 ± 10.1 | 0.91 | 1.6 ± 0.4 | 1.2 | 50 |
| Iodo[Tyr10]OFQ/N (1–11) | 38.9 ± 5.9 | 0.93 | 0.58 ± 0.16 | 0.88 | 67 |
| OFQ/N (1–7) | 360 ± 110 | 0.70 | 440 ± 134 | 0.83 | 0.8 |
| Opioid peptides | |||||
| Dynorphin A (1–17) | 72.8 ± 22 | 0.98 | 6.0 ± 0.7 | 0.88 | 12 |
| Dynorphin B (1–13) | 247 ± 10 | 1.1 | 33.9 ± 8.3 | 0.74 | 7 |
| α-Neoendorphin | 192 ± 14 | 1.3 | 6.5 ± 1.5 | 0.89 | 30 |
| [Met5]Enkephalin | >1000 | >1000 | |||
| [Leu5]Enkephalin | >1000 | >1000 | |||
| DAMGO | >1000 | >1000 | |||
| DPDPE | >1000 | >1000 | |||
| Opiates | |||||
| Morphine | >1000 | >1000 | |||
| Naltrindole | >5000 | 236 ± 74 | 0.76 | >21 | |
| Nor-binaltorphimine | >7500 | 898 ± 217 | 0.58 | >8.4 | |
| Naltrexone | >1000 | >1000 | |||
| Naloxone | >1000 | >1000 | |||
| NalBzoH | 358 ± 57 | 0.79 | 3.9 ± 0.2 | 0.99 | 92 |
| Fentanyl | >5000 | 39.6 ± 5.0 | 0.82 | >126 | |
| (−)Cyclazocine | >7500 | 157 ± 11.5 | 0.84 | >48 | |
| (+)Cyclazocine | >1000 | >1000 | |||
| Levallorphan | >5000 | 266 ± 12 | 0.52 | >19 | |
| Diprenorphine | >4000 | 312 ± 76 | 0.55 | >13 | |
| (−)Pentazocine | >1000 | >1000 | |||
| (+)Pentazocine | >1000 | >1000 | |||
| U50,488H | >1000 | >1000 | |||
Data adapted from Mathis et al. (1997, 1999).