N-arylalkylpiperidines as high-affinity sigma-1 and sigma-2 receptor ligands:: Phenylpropylamines as potential leads for selective sigma-2 agents
N-arylalkylpiperidines as high-affinity sigma-1 and sigma-2 receptor ligands:: Phenylpropylamines as potential leads for selective sigma-2 agents
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DOI：
10.1016/s0960-894x(01)00788-0
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发表时间：
2002-02-11
影响因子：
2.7
通讯作者：
Coop, A
中科院分区：
文献类型：
--
作者：
Maeda, DY;Williams, W;Coop, A
为了描述在sigma-1和sigma-2受体上识别所需的结构要求之间的差异，在结合试验中评价了一系列苯乙基和苯丙基哌啶。发现苯乙基哌啶有利于σ-1受体，而苯丙哌啶倾向于有利于σ-2受体。看来苯丙胺是选择性σ-2配体的潜在药效团。(C)2002爱思唯尔科技有限公司版权所有。
To delineate the differences between the structural requirements necessary for recognition at sigma-1 and sigma-2 receptors, a range of phenethyl- and phenylpropylpiperidines were evaluated in binding assays. Phenethylpiperidines were found to favor sigma-1 receptors, whereas phenylpropylpiperidines tend to favor sigma-2 receptors. It appears that phenylpropylamine is a potential pharmacophore for selective sigma-2 ligands. (C) 2002 Elsevier Science Ltd. All rights reserved.