Opioid compounds with mixed mu 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 p selective agonist endomorphin-2 and the delta selective antagonist pharmacophore Dmt-Tic. As predicted, the resulting bivalent ligand showed a p agonist/delta antagonist profile deriving fi-om the corresponding activities of each pharmacophore. (C) 2007 Elsevier Ltd. All rights reserved.

A new opioid designed multiple ligand derived from the mu opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic / S., Salvadori; C., Trapella; S., Fiorini; Negri, Lucia; Lattanzi, Roberta; S. D., Bryant; Y., Jinsmaa; L. H., Lazarus; G., Balboni. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - STAMPA. - 15:(2007), pp. 6876-6881. [10.1016/j.bmc.2007.08.047]

A new opioid designed multiple ligand derived from the mu opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic

NEGRI, Lucia;LATTANZI, Roberta;
2007

Abstract

Opioid compounds with mixed mu 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 p selective agonist endomorphin-2 and the delta selective antagonist pharmacophore Dmt-Tic. As predicted, the resulting bivalent ligand showed a p agonist/delta antagonist profile deriving fi-om the corresponding activities of each pharmacophore. (C) 2007 Elsevier Ltd. All rights reserved.
2007
analgesia; delta opioid receptors; designed multiple ligand; dmt-tic pharmacophore; endomorphin-2; mu opioid receptors; opioid peptides; physical dependence
01 Pubblicazione su rivista::01a Articolo in rivista
A new opioid designed multiple ligand derived from the mu opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic / S., Salvadori; C., Trapella; S., Fiorini; Negri, Lucia; Lattanzi, Roberta; S. D., Bryant; Y., Jinsmaa; L. H., Lazarus; G., Balboni. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - STAMPA. - 15:(2007), pp. 6876-6881. [10.1016/j.bmc.2007.08.047]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/235912
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