Table 5 Bioactivity of Dmt-Tic and Dmt-Tic-Ala opioidmimetic peptides
Peptide | MVD—Antagonist Activity (nM) | GPI—Agonist Activity (μM) | ||
|---|---|---|---|---|
pA2 | K e | pA2 | IC50 | |
Naltrindole | 9.2 | 0.7 | 7.3 | 0.053 |
1. Dmt-Tic-OH | 8.2 | 5.7 | — | >10 |
2. Dmt-Tic-NH2 | 7.2 | 42 | — | >10 |
5. Dmt-Tic-CH2OH | 7.0 | 66 | — | >10 |
11. Dmt-Tic-Ala-OH | 8.4 | 4 | — | >10 |
12. Dmt-Tic-Ala-NH2 | 8.0 | 9 | — | 4.74 ± 0.9 |