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EnglishOpioid 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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| Titolo: | A new opioid designed multiple ligand derived from the mu opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic | |
| Autori: | ||
| Data di pubblicazione: | 2007 | |
| Rivista: | ||
| Abstract: | Opioid 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. | |
| Handle: | http://hdl.handle.net/11584/22951 | |
| Tipologia: | 1.1 Articolo in rivista |
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http://hdl.handle.net/11584/22951
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