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. 2020 Dec 22;22(1):20. doi: 10.3390/ijms22010020

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.