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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
