Trifluoromethoxyl substituted phenylethylene diamines as high affinity sigma receptor ligands with potent anti-cocaine actions.
Trifluoromethoxyl substituted phenylethylene diamines as high affinity sigma receptor ligands with potent anti-cocaine actions.
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DOI：
10.1021/jm7013666
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发表时间：
2008-05
影响因子：
7.3
通讯作者：
T. A. Smith;Xiaowen Yang;Huifang Wu;B. Pouw;R. Matsumoto;A. Coop
中科院分区：
文献类型：
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作者：
T. A. Smith;Xiaowen Yang;Huifang Wu;B. Pouw;R. Matsumoto;A. Coop
苯乙烯二胺是一类σ受体配体，其对其他生物系统具有优异的选择性，并且具有涉及σ 1受体拮抗作用的抗可卡因作用。为了增加芳族甲氧基取代的类似物的效力，引入三氟甲氧基以防止代谢去甲基化。对位取代的三氟甲氧基取代的类似物显示出具有增加的σ受体亲和力，并且代表了迄今为止描述的最有效的抗可卡因苯乙烯二胺。
The phenylethylene diamines are a class of sigma receptor ligands with excellent selectivity over other biological systems and with anti-cocaine actions that involve antagonism of sigma1 receptors. In order to increase the potency of the aromatic methoxyl substituted analogues, trifluoromethoxyl groups were introduced to prevent metabolic demethylation. The para-substituted trifluoromethoxyl substituted analogues were shown to have increased sigma receptor affinity and represent the most potent anti-cocaine phenylethylene diamines yet described.