• Corpus ID: 21320896

Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.

  title={Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.},
  author={Gianfranco Balboni and Severo Salvadori and Remo Guerrini and Lucia Negri and Elisa Giannini and Yunden Jinsmaa and Sharon D. Bryant and Lawrence H. Lazarus},
  journal={Journal of medicinal chemistry},
  volume={45 25},
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 a third heteroaromatic nucleus, such as 1H-benzimidazole-2-yl (Bid) and a linker of specified length both located C-terminally to Tic in the general formula H-Dmt-Tic-NH-CH(R)-R'. The distance between Tic and Bid is a determining factor responsible for the acquisition of delta agonism (2, 2', 3, 4… 

Pentapeptides displaying mu opioid receptor agonist and delta opioid receptor partial agonist/antagonist properties.

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Modulation of Opioid Receptor Ligand Affinity and Efficacy Using Active and Inactive State Receptor Models

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Hydrogen Sulfide Increases the Analgesic Effects of µ- and δ-Opioid Receptors during Neuropathic Pain: Pathways Implicated

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Development of new opioid ligands possessing mixed μ agonist/δ agonist profile and mixed μ receptor agonists as well as δ receptor antagonists profile has emerged as a promising new approach to analgesic drug development.

In vitro and in vivo pharmacological profile of UFP‐512, a novel selective δ‐opioid receptor agonist; correlations between desensitization and tolerance

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Effect of δ-Opioid Receptor Activation on BDNF-TrkB vs. TNF-α in the Mouse Cortex Exposed to Prolonged Hypoxia

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