Ki (nM) | |||||
---|---|---|---|---|---|
Peptide | R | R′ | δ | μ | μδ |
Dipeptides | |||||
1. Dmt-Tic | OH | 0.022 ± 0.0015 (6) | 3,317 ± 435 (7) | 150,773 | |
2. Dmt-Tic | NH2 | 1.22 ± 0.09 (6) | 276.8 ± 26.9 (3) | 227 | |
3. Dmt-d-Tic | OH | 13.5 ± 1.59 (4) | 224.4 ± 25.6 (3) | 17 | |
4. Dmt-d-Tic | NH2 | 56.9 ± 2.90 (3) | 3.8 ± 0.24 (3) | 0.067 | |
5. Dmt-Tic | CH2OH | 0.44 ± 0.14 (6) | 151.4 ± 16.3 (3) | 344 | |
6. Tyr-Tic | OH | 191.7 ± 47.8 (7) | 28,411 ± 2,941 (3) | 148 | |
7. Tyr-Tic | NH2 | 165.9 ± 48.1 (4) | 28,712 ± 3,305 (7) | 173a | |
8. Tyr-d-Tic | OH | 9,046 ± 719 (5) | 26,258 ± 427 (3) | 2.9 | |
9. Tyr-d-Tic | NH2 | 5,959 ± 981 (4) | 3,135 ± 491 (4) | 0.53a | |
10. Tyr-Tic | CH2OH | 128.1 ± 34.7 (4) | 11,003 ± 1,851 (3) | 86 | |
Tripeptides | |||||
11. Dmt-Tic | Ala | OH | 0.285 ± 0.03 (6) | 5,813 ± 675 (4) | 20,396 |
12. Dmt-Tic | Ala | NH2 | 0.241 ± 0.02 (5) | 47.1 ± 3.4 (4) | 195 |
13. Dmt-d-Tic | Ala | OH | 88.7 ± 13.8 (5) | 82.8 ± 2.0 (3) | 0.93 |
14. Dmt-d-Tic | Ala | NH2 | 46.4 ± 2.7 (3) | 5.8 ± 0.85 (4) | 0.13 |
15. Tyr-Tic | Ala | OH | 56.1 ± 10.3 (3) | 8,291 ± 1,377 (3) | 148a |
16. Tyr-Tic | Ala | NH2 | 55.5 ± 13.7 (3) | 33,844 ± 1,405 (3) | 610a |
17. Tyr-d-Tic | Ala | OH | 2,346 ± 356 (3) | 14,028 ± 2,166 (3) | 6 |
18. Tyr-d-Tic | Ala | NH2 | 21,076 ± 4,427 (3) | 8,146 ± 1,377 (3) | 0.39a |