The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands

被引:10
|
作者
Jong, L [1 ]
Zaveri, N [1 ]
Toll, L [1 ]
机构
[1] SRI Int, Biosci Div, Menlo Pk, CA 94025 USA
关键词
D O I
10.1016/j.bmcl.2003.09.068
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A new class of high affinity opioid and opioid receptor-like receptor (ORL1 receptor, NOP receptor) ligands has been designed by conformational restriction of piperidine-based NOP receptor ligands, resulting in a novel quinolizidine scaffold. Different modifications of the pendant functional groups on the scaffold provide differential activities at the opioid and NOP receptors. While the conformational rigidity will provide an improved understanding of the NOP and opioid receptor binding pockets, these compounds also provide a new template for the design of novel opiate and NOP ligands. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:181 / 185
页数:5
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