A bivalent ligand (KDAN-18) containing δ-antagonist and k-agonist pharmacophores bridges δ2 and k1 opioid receptor phenotypes

被引：98

作者：

Daniels, DJ ^{[1
]}

Kulkarni, A ^{[1
]}

Xie, ZH ^{[1
]}

Bhushan, RG ^{[1
]}

Portoghese, PS ^{[1
]}

机构：

[1] Univ Minnesota, Coll Pharm, Dept Med Chem, Minneapolis, MN 55455 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 06期

关键词：

D O I：

10.1021/jm034234f

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

To characterize delta- and kappa-opioid receptor phenotypes, bivalent ligands (KDAN series) containing delta-antagonist (naltrindole) and kappa(1)-agonist (ICI-199,441) pharmacophores were synthesized and evaluated by the intrathecal route using the mouse tail-flick assay and binding studies. The data have suggested that KDAN-18 (2) bridges phenotypic delta(2)- and kappa(1)-receptors. A conceptual model is presented to explain the organizational differences between the opioid receptors that give rise to the phenotypes (delta(1), delta(2), kappa(1), kappa(2)).

引用

页码：1713 / 1716

页数：4

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