The tetrapeptide DALDA (H-Tyr-d-Arg-Phe-Lys-NH2) is a polar and selective μ agonist
showing poor penetration of the placental and blood–brain barriers. In an effort to enhance …

[Dmt1] DALDA (H-Dmt-d-Arg-Phe-Lys-NH2; Dmt= 2′, 6′-dimethyltyrosine) binds with high
affinity and selectivity to the μ opioid receptor and is a surprisingly potent and long-acting …

Recent evidence suggests that highly selective μ-opioid agonists may provide good
analgesia with less development of tolerance and dependence. H-Tyr-d-Arg-Phe-Lys-NH2 …

Two recent developments of opioid peptide-based analgesics are reviewed. The first part of
the review discusses the dermorphin-derived, cationic-aromatic tetrapeptide H-Dmt-D-Arg …

DALDA (H-Tyr-d-Arg-Phe-Lys-NH2) and [Dmt1] DALDA (H-Dmt-d-Arg-Phe-Lys-NH2)(Dmt=
2′, 6′-dimethyltyrosine) are potent and highly selective μ-opioid agonists (K i δ/K i μ> …

Analogues of the 2 ', 6 '-dimethyl-l-tyrosine (Dmt)− 1, 2, 3, 4-tetrahydroisoquinoline-3-
carboxylic acid (Tic) pharmacophore were prepared to test the hypothesis that a “spacer” …

Recent studies showed that dermorphin and enkephalin analogues containing two methyl
groups at the 2 ', 6 '-positions of the Tyr aromatic ring and lacking an N-terminal amino group …

The single amino acid replacement of 2′, 6′-dimethyl-l-tyrosine in deltorphin B (H-Dmt-d-
Ala-Phe-Glu-Val-Val-Gly-NH2) yielded high affinity for μ-and δ-binding sites.[Dmt1] …

The introduction of the Dmt (2′, 6′‐dimethyl‐l‐tyrosine)–Tic pharmacophore into the
design of opioid ligands produced an extraordinary family of potent δ‐opioid receptor …

Abstract Background Tyr-Tic (1, 2, 3, 4-tetrahydroisoquinoline-3-carboxylic acid) and Tyr-Tic-
Ala were the first peptides with δ opioid antagonist activity lacking Phe, considered essential …