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Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
The data demonstrate that a linker separating the Dmt-Tic pharmacophore and Bid, regardless of the presence of a negative charge, is important in the acquisition of opioids exhibiting potent delta agonism and weak mu agonism from a parent delta antagonist. Expand
Synthesis of stereoisomeric analogues of endomorphin-2, H-Tyr-Pro-Phe-Phe-NH(2), and examination of their opioid receptor binding activities and solution conformation.
- Y. Okada, A. Fukumizu, +5 authors L. Lazarus
- Chemistry, Medicine
- Biochemical and biophysical research…
- 16 September 2000
The data clearly indicated that the three dimensional structure of endomorphin-2 with the natural l-configuration was the most suitable for binding within the mu receptor, but specific residues are important for activity. Expand
δ Opioidmimetic Antagonists: Prototypes for Designing a New Generation of Ultraselective Opioid Peptides
Dmt-Tic opioidmimetic peptides represent a highly potent class of opioid peptide antagonists with greater potency than the nonopioid δ antagonist naltrindole and have potential application as clinical and therapeutic compounds. Expand
Evaluation of the Dmt-Tic pharmacophore: Conversion of a potent δ-opioid receptor antagonist into a potent δ agonist and ligands with mixed properties
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” and a third aromatic center… Expand
Potent δ-Opioid Receptor Agonists Containing the Dmt−Tic Pharmacophore
Conversion of delta-opioid receptor antagonists containing the 2',6'-dimethyl-L-tyrosine (Dmt)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (Tic) pharmacophore into potent delta-agonists required… Expand
Endomorphins and related opioid peptides.
Opioidmimetics and opioid peptides containing the amino acid sequence of the message domain of endomorphins, Tyr-Pro-Phe/Trp, could exhibit unique binding activity and lead to the development of new therapeutic drugs for controlling pain. Expand
Bifunctional [2‘,6‘-Dimethyl-l-tyrosine1]endomorphin-2 Analogues Substituted at Position 3 with Alkylated Phenylalanine Derivatives Yield Potent Mixed μ-Agonist/δ-Antagonist and Dual…
Endomorphin-2 (H-Tyr-Pro-Phe-Phe-NH2) and [Dmt1]EM-2 (Dmt = 2‘,6‘-dimethyl-l-tyrosine) analogues, containing alkylated Phe3 derivatives, 2‘-monomethyl (2, 2‘), 3‘,5‘- and 2‘,6‘-dimethyl (3, 3‘, and… Expand
Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties.
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" and a third aromatic center… Expand
Dmt and opioid peptides: A potent alliance
An overview of the crucial role played by the Dmt–Tic residue in the proliferation of opioid peptides with high receptor affinity (Ki equal to or less than 1 nM) and potent bioactivity is documented. Expand
Development of Potent Bifunctional Endomorphin-2 Analogues with Mixed μ-/δ-Opioid Agonist and δ-Opioid Antagonist Properties
The C terminus of endomorphin-2 (EM-2) analogues (Tyr-Pro-Phe-NH-X) was modified with aromatic, heteroaromatic, or aliphatic groups (X = phenethyl,benzyl, phenyl, naphthyl, pyridyl, quinolyl,… Expand