Acta Biochimica Polonica 2001-01-01

DALDA analogues containing alpha-hydroxymethylamino acids.

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

文献索引：Acta Biochim. Pol. 48(4) , 1121-4, (2001)

全文：HTML全文

摘要

To evaluate the role of aromatic amino-acids residues, four analogues of the mu-selective opioid peptide agonist DALDA (H-Tyr-D-Arg-Phe-Lys-NH2) containing the amphiphilic, a,a-disubstituted amino acid (R)- or (S)-alpha-hydroxymethyltyrosine (HmTyr) in position 1 and (R)- or (S)-alpha-hydroxymethylphenylalanine (HmPhe) 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 delta receptor-selective opioid agonist.