EN
To evaluate the role of aromatic amino-acids residues, four analogues of theu-selective opioid peptide agonist DALDA (H-Tyr-D-Arg-Phe-Lys-NH2) containing the amphiphilic, a,a-disubstituted amino acid (R)- or (S)-a-hydroxymethyltyrosine (HmTyr) in position 1 and (R)- or (S)-a-hydroxymethylphenylalanine (Hm3Phe) in position 3 of the peptide sequence were synthesized. Only the [(R)- HmPhe3)]DALDA analogue displayed full agonistic activity in both the guinea pig ileum and the mouse vas deferens assays and turned out to be a δ receptor-selective opioid agonist.