• Corpus ID: 21320896

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

@article{Balboni2002PotentDR,
  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},
  year={2002},
  volume={45 25},
  pages={
          5556-63
        }
}
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… 

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