Smith Trudy A, Yang Xiaowen, Wu Huifang, Pouw Buddy, Matsumoto Rae R, Coop Andrew
Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD 21201, USA.
J Med Chem. 2008 Jun 12;51(11):3322-5. doi: 10.1021/jm7013666. Epub 2008 May 8.
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.
苯乙二胺是一类对其他生物系统具有优异选择性的σ受体配体,具有涉及拮抗σ1受体的抗可卡因作用。为了提高芳基甲氧基取代类似物的效力,引入了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类似物显示出增加的σ受体亲和力,是迄今所描述的最有效的抗可卡因苯乙二胺。