Trifluoromethoxyl Substituted Phenylethylene Diamines as High Affinity σ Receptor Ligands with Potent Anti-Cocaine Actions

详细信息    查看全文

• 作者：Trudy A. Smith ; Xiaowen Yang ; Huifang Wu ; Buddy Pouw ; Rae R. Matsumoto ; Andrew Coop
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：June 12, 2008
• 年：2008
• 卷：51
• 期：11
• 页码：3322 - 3325
• 全文大小：79K
• 年卷期：v.51,no.11(June 12, 2008)
• ISSN：1520-4804

文摘

The phenylethylene diamines are a class of σ receptor ligands with excellent selectivity over other biological systems and with anti-cocaine actions that involve antagonism of σ₁ 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 σ receptor affinity and represent the most potent anti-cocaine phenylethylene diamines yet described.