Table 1.
Opioid activity of the screened deltorphin analogues.
| Sequence | % Inhibition at DOR 100 nM, 1 µM |
% Inhibition at MOR 100 nM, 1 µM |
Ki DOR (nM) | Ki MOR (nM) | Ki KOR (nM) | |
|---|---|---|---|---|---|---|
| DPDPE | 72, 84 | 23, 62 | 4.3 | 180 | ||
| H2N-YaFDVVG-S(β-D-Glc)-G | LSZ-27 | 51, 67 | 6, 48 | 33 | 570 | |
| H2N-YmFHLM-S(β-D-Glc) | BBI-11001 | 72, 84 | 63, 89 | |||
| H2N-YaFHLA-S(β-D-Glc) | BBI-11002 | 55, 77 | 82, 97 | |||
| H2N-YmFHLMT-(β-D-Glc) | BBI-11003 | 75, 83 | 57, 89 | |||
| H2N-YaFHLAT-(β-D-Glc) | BBI-11004 | 61, 76 | 88, 98 | |||
| H2N-YaFE-Nva-Nva-S-(β-D-Glc) | BBI-11005 | 65, 80 | 11, 44 | 20 | 710 | 5.3% |
| H2N-YaFE-Nle-Nle-S-(β-D-Glc) | BBI-11006 | 66, 81 | 7, 42 | 11 | 820 | 38% |
| H2N-YaFE-Nva-Nva-T-(β-D-Glc) | BBI-11007 | 64, 80 | 13, 36 | 16 | 1300 | 0% |
| H2N-YaFE-Nle-Nle-T-(β-D-Glc) | BBI-11008 | 74, 84 | 7, 37 | 14 | 1100 | 2.9% |
| H2N-YaFE-Nle-Nle-T | BBI-11009 | 11 | 510 | 3.7% | ||
| H2N-YaFEII-T-(β-D-Glc) | BBI-11014 | 80 | 2600 | 36% | ||
| H2N-YaFEVV-S-(β-D-Glc) | BBI-11015 | 320 | 1500 | 0% | ||
| H2N-YaFE-Nle-Nle-S-(βGlc-βGal) | BBI-11021 | 17 | 1500 | 23% | ||
| H2N-YaFEVV-S-(βGlc-βGal) | BBI-11022 | 3600 | 1000 | 71% | ||
| H2N-YaFE-Nle-Nle-S-(α-D-Man) | BBI-11023 | 8.2 | 840 | 4.7% | ||
| H2N-YaFE-Nva-Nva-S-(α-D-Man) | BBI-11024 | 13 | 990 | 0% | ||
| H2N-YaFE-Nle-Nle-S-(βGlc-βGlc) | BBI-11025 | 13 | 1200 | 46% | ||
| H2N-YaFE-Ile-Ile-S-(βGlc-βGlc) | BBI-11026 | 61 | 3000 | 2.7% |
Nva = nor-Valine, Nle = nor-Leucine, Glc = Glucose, Gal = Galactose, Man = Mannose.