The effect of the pyridyl nitrogen position in pyridylpiperazine sigma ligands.

The effect of the pyridyl nitrogen position in pyridylpiperazine sigma ligands.
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DOI:
10.1016/j.bmcl.2010.02.087
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发表时间:
2010-04-15
影响因子:
2.7
通讯作者:
Coop, Andrew
Coop, Andrew
中科院分区:
医学4区
文献类型:
--
作者:
Stavitskaya, Lidiya;Seminerio, Michael J.;Matthews-Tsourounis, Marilyn M.;Matsumoto, Rae R.;Coop, Andrew

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合成了一系列吡啶基哌嗪,并对其与σ1和σ2受体的结合亲和力进行了分析,确定了对σ1和σ2受体识别的最佳吡啶基氮位置和链长。(3-吡啶基)哌嗪和(4-吡啶基)哌嗪倾向于σ1受体,而先前研究的(2-吡啶基)哌嗪倾向于σ2受体。
A series of pyridylpiperazines was synthesized and analyzed for sigma receptor binding affinity to determine the optimal pyridyl nitrogen position and chain length for the σ1 and σ2 receptor recognition. The (3-pyridyl)piperazines and (4-pyridyl)piperazines favor σ1 receptors, while previously studied (2-pyridyl)piperazines favor σ2 receptors.
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