Table 2.
Opioid binding affinities of Dyn B amide alanine analogs.
| Tyr1-Gly-Gly-Phe4-Leu5-Arg6-Arg7-Gln8-Phe9-Lys10-Val11-Val-Thr-NH2 | ||||
|---|---|---|---|---|
|
| ||||
| Compound | Ki (nM ± SEM)a | |||
| KOR | MOR | DOR | KOR/MOR/DOR | |
| N-Terminal alanine substituted analogs | ||||
| 1 [Ala1] | 886 ± 123 | 651 ± 70 | >10,000 | 1/0.7/>11 |
| 2 [Ala4] | 1510 ± 221 | 1040 ± 100 | >10,000 | 1/0.7/>6 |
| C-Terminal alanine substituted analogs | ||||
| 3 [Ala5] | 12.1 ± 5.2 | 20.3 ± 3.1 | 265 ± 43 | 1/2/22 |
| 4 [Ala6] | 43.1 ± 2.8 | 14.1 ± 3.0 | 25.7 ± 1.6 | 1/0.3/0.6 |
| 5 [Ala7] | 82.4 ± 9.3 | 16.7 ± 5.1 | 67.5 ± 8.3 | 1/0.2/0.8 |
| 6 [Ala8] | 13.0 ± 0.96 | 4.32 ± 0.10 | 54.0 ± 6.9 | 1/0.3/4 |
| 7 [Ala9] | 11.3 ± 1.7 | 3.76 ± 0.22 | 42.1 ± 2.5 | 1/0.3/4 |
| 8 [Ala10] | 31.6 ± 6.0 | 40.5 ± 3.9 | 119 ± 16 | 1/0.8/4 |
| 9 [Ala11] | 12.4 ± 1.6 | 7.45 ± 2.69 | 58.8 ± 3.4 | 1/0.6/5 |
| Dyn B amide | 6.30 ± 1.68 | 8.05 ± 2.87 | 43.2 ± 1.6 | 1/1.3/7 |
a
Values are mean ± SEM for n ≥ 3.