Table 1.
| ||||||||||
---|---|---|---|---|---|---|---|---|---|---|
Compd | R1 | R2 | R3 | R4 | R5 | Ke (nM)
|
μ/κ | δ/κ | ||
DAMGO, μ | DPDPE, δ | U69,593, κ | ||||||||
2 (nor-BNI) | 26 | 29 | 0.05 | 520 | 580 | |||||
3 (JDTic) | H | OH | H | H | H | 3.41 | 79.3 | 0.01 | 341 | 7930 |
23a | CH3 | OH | H | H | H | 51 | 118 | 0.06 | 850 | 1966 |
23b | H | OCH3 | H | H | H | 24 | 21.2 | 0.037 | 649 | 573 |
23c | H | OH | CH3 | H | H | 3 | 24 | 0.03 | 100 | 800 |
23d | H | OH | H | CH3 | H | 3.6 | 854 | 0.03 | 120 | 28500 |
23e | H | OH | H | H | CH3 | 210 | 491 | 0.16 | 1313 | 3070 |
23f | H | CONH2 | H | H | H | 21 | 480 | 0.12 | 175 | 400 |