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

被引：26
作者：
Salvadori, Severo
Trapella, Claudio
Fiorini, Stella
Negri, Lucia
Lattanzi, Roberta
Bryant, Sharon D.
Jinsmaa, Yunden
Lazarus, Lawrence H.
Balboni, Gianfranco [1 ]
机构：
[1] Univ Ferrara, Ctr Biotechnol, Dept Pharmaceut Sci, I-44100 Ferrara, Italy
[2] Univ Roma La Sapienza, Dept Human Physiol & Pharmacol, I-00185 Rome, Italy
[3] NIEHS, Lab Pharmacol & Chem, Med Chem Grp, Res Triangle Pk, NC 27709 USA
[4] Univ Cagliari, Dept Toxicol, I-09126 Cagliari, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 22期
关键词：
designed multiple ligand; endomorphin-2; Dmt-Tic pharmacophore; analgesia; physical dependence; opioid peptides; delta opioid receptors; mu opioid receptors;
D O I：
10.1016/j.bmc.2007.08.047
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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.
引用
收藏
页码：6876 / 6881
页数：6
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