Binding affinity (Ki) values of selected compounds to opioid receptors
Values represent the mean ± S.E.M. of at least three independent determinations.
Compound | Ki (nM) | ||||||
|---|---|---|---|---|---|---|---|
| ORL-1 | μ | δ | κ | ||||
| Nociceptin | 0.079 ± 0.021 | 128.5 ± 7.5 | >2500 | 49.4 ± 9.3 | |||
| SB-612111 | 0.33 ± 0.03 | 57.6 ± 8.0 | 2109 ± 570 | 160.5 ± 22.4 | |||
| SB-612112 | 1.3 ± 0.23 | 34.5 ± 5.0 | >2500 | 161 ± 4 | |||
| JTC-801 | 30.8 ± 3.0 | 93.3 ± 32.1 | >2500 | 1659 ± 400 | |||
| (-)-J-113397 | 157 ± 41 | 33.7 ± 2.9 | >2500 | 198 ± 16 | |||
| (+)-J-113397 | 2.0 ± 0.7 | 30.7 ± 7.6 | >2500 | 58.3 ± 6.9 | |||
| DAMGO | >10,000 | 0.58 ± 0.03 | 1260 ± 195 | 185 ± 13 | |||
| Morphine | >10,000 | 0.70 ± 0.07 | 336 ± 102 | 27.1 ± 4.0 | |||
| DPDPE | >5000 | 200 ± 35.8 | 6.1 ± 0.6 | >10,000 | |||
| BRL 52656 | >10,000 | 371 ± 32 | >2500 | 0.14 ± 0.03 | |||
| U-69593 | >10,000 | 510 ± 61 | >2500 | 0.37 ± 0.06 | |||
| Naloxone | >10,000 | 0.42 ± 0.05 | 38.7 ± 9.9 | 1.21 ± 0.10 | |||