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- Severo Salvadori, Claudio Trapella, Stella Fiorini, Lucia Negri, Roberta Lattanzi, Sharon D Bryant, Yunden Jinsmaa, Lawrence H Lazarus, and Gianfranco Balboni.
- Department of Pharmaceutical Science and Biotechnology Center, University of Ferrara, I-44100 Ferrara, Italy.
- Bioorg. Med. Chem. 2007 Nov 15;15(22):6876-81.
AbstractOpioid compounds with mixed micro agonist/delta antagonist properties could be used as analgesics with low propensity to induce tolerance and dependence. Here we report the synthesis of a new designed multiple ligand deriving from the micro selective agonist endomorphin-2 and the delta selective antagonist pharmacophore Dmt-Tic. As predicted, the resulting bivalent ligand showed a micro agonist/delta antagonist profile deriving from the corresponding activities of each pharmacophore.
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