Characteristics of opioid compounds in equilibrium displacement binding of [3H]DAMGO (mu), [3H]p-CI-DPDPE (delta), [3H]U69,593 (kappa-1) and [3H]bremazocine (kappa-all) sites
| Compound | Ki | Selectivity | ||||||
|---|---|---|---|---|---|---|---|---|
| mu | delta | kappa-1 | kappa-all | mu:delta | mu:kappa-1 | mu:kappa-all | kappa-1:kappa-all | |
| nM | ||||||||
| Alfentanil | 23 | >105 | 161,000 | >104 | >4000 | 7000 | >400 | >0.06 |
| Butorphanol | 0.5 | 17 | 0.68 | 6.1 | 34 | 1.4 | 12 | 9.0 |
| DAMGO | 3.3 | 1347 | 1311 | 14,874 | 408 | 397 | 4507 | 11 |
| Etonitazene | 0.17 | 275 | 399 | 1556 | 1618 | 2347 | 9153 | 3.9 |
| Morphine | 5.6 | 389 | 247 | 1534 | 69 | 44 | 274 | 6.2 |
| Nalbuphine | 1.4 | 244 | 8.5 | 370 | 174 | 6.1 | 264 | 44 |
| BWB373 | 15 | 0.23 | 30 | 218 | 0.02 | 2.0 | 15 | 7.3 |
| DPDPE | 1348 | 2.4 | 558 | 2534 | 0.002 | 0.41 | 1.9 | 4.5 |
| Bremazocine | N.D. | N.D. | 0.15 | 0.39 | N.D. | N.D. | N.D. | 2.6 |
| CI-977 | 17 | 1051 | 0.16 | 1.7 | 62 | 0.01 | 0.1 | 11 |
| DYN A(1–13) | 30 | 106 | 0.44 | 1.4 | 3.5 | 0.01 | 0.05 | 3.2 |
| DYN A(1–17) | 14 | 129 | 0.16 | 2.9 | 9 | 0.01 | 0.21 | 18 |
| E-2078 | 10 | 140 | 0.37 | 2.5 | 14 | 0.04 | 0.25 | 6.8 |
| EKC | 1.7 | 25 | 1.2 | 3.6 | 15 | 0.71 | 2.1 | 3.0 |
| nor-BNI | 14 | 36 | 0.28 | 0.63 | 3 | 0.02 | 0.05 | 2.3 |
| U50,488 | N.D. | N.D. | 0.89 | 14 | N.D. | N.D. | N.D. | 16 |
| U69,593 | 208 | 10,853 | 1.3 | 49 | 52 | 0.01 | 0.24 | 38 |
N.D., not determined.