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DALDA analogues containing alpha-hydroxymethylamino acids

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Olma A., Chung N. N., Schiller P. W., Zabrocki J.

Acta Biochimica Polonica

2001

tom 48

nr 4

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.

Ograniczanie wyników

1 Acta Biochimica Polonica

1 Chung N. N.

1 Olma A.

1 Schiller P. W.

1 Zabrocki J.

1 2001

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DALDA analogues containing alpha-hydroxymethylamino acids