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={G. Balboni and S. Salvadori and R. Guerrini and L. Negri and E. Giannini and Y. Jinsmaa and S. Bryant and L. 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… Expand
Histogranin-Like Antinociceptive and Anti-Inflammatory Derivatives of o-Phenylenediamine and Benzimidazole
Molecular Pharmacology of δ-Opioid Receptors
Effect of δ-Opioid Receptor Activation on BDNF-TrkB vs. TNF-α in the Mouse Cortex Exposed to Prolonged Hypoxia
Agonists at the δ‐opioid receptor modify the binding of µ‐receptor agonists to the µ–δ receptor hetero‐oligomer