Biochemical and Biophysical Research Communications
[D-ALA2]deltorphin II analogs with high affinity and selectivity for delta-opioid receptor
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Pharmacology of a new tritiated endomorphin-2 analog containing the proline mimetic cis-2-aminocyclohexanecarboxylic acid
2011, PeptidesCitation Excerpt :The Ki of [(1S,2R)ACHC]2EM-2 agreed well with its KD value obtained in saturation experiments. The δ-selective Ile5,6-deltorphin-2 [33] and the κ-specific benzeneacetamide derivative U-50,488H [22] proved to be poor inhibitors of the radioligand. The distribution of the binding sites labeled with [3H][(1S,2R)ACHC]2EM-2 was examined by receptor autoradiography in rat brain coronal sections (Fig. 5).
Exploring deltorphin II binding to the third extracellular loop of the δ-opioid receptor
2004, Journal of Biological ChemistryCitation Excerpt :One can conclude from these data that there is some hydrophobic interaction between Leu295, Val296, and Val297 of hDOR-(281–297) and the C-terminal address domain of deltorphin II (deltorphin II Val5–Gly7). Indeed, many groups have reported that the hydrophobicity associated with Val5 and Val6 is critical for δ-opioid receptor binding and selectivity (13–15). Therefore, it is possible that Val5 and Val6 of deltorphin II interact with the Leu295–Val297 segment of hDOR.
Dermorphin and deltorphin heptapeptide analogues: Replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity
2002, Bioorganic and Medicinal Chemistry LettersCitation Excerpt :All peptides were synthesized (Tables 1 and 2) by a solid-phase method using Fmoc chemistry, as previously described.16,20