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

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.

journal_name

Bioorg Med Chem

authors

Salvadori S,Trapella C,Fiorini S,Negri L,Lattanzi R,Bryant SD,Jinsmaa Y,Lazarus LH,Balboni G

doi

10.1016/j.bmc.2007.08.047

subject

Has Abstract

pub_date

2007-11-15 00:00:00

pages

6876-81

issue

22

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(07)00726-2

journal_volume

15

pub_type

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