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 Chemjournal_title
Bioorganic & medicinal chemistryauthors
Salvadori S,Trapella C,Fiorini S,Negri L,Lattanzi R,Bryant SD,Jinsmaa Y,Lazarus LH,Balboni Gdoi
10.1016/j.bmc.2007.08.047subject
Has Abstractpub_date
2007-11-15 00:00:00pages
6876-81issue
22eissn
0968-0896issn
1464-3391pii
S0968-0896(07)00726-2journal_volume
15pub_type
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