Conversion of a Highly Selective Sigma-1 Receptor–Ligand to Sigma-2 Receptor Preferring Ligands with Anticocaine Activity
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- 作者：Christophe Mé ; sangeau ; Sanju Narayanan ; Andrea M. Green ; Jamaluddin Shaikh ; Nidhi Kaushal ; Eddy Viard ; Yan-Tong Xu ; James A. Fishback ; Jacques H. Poupaert ; Rae R. Matsumoto ; Christopher R. McCurdy
- 刊名：Journal of Medicinal Chemistry
- 出版年：2008
- 出版时间：March 13, 2008
- 年：2008
- 卷：51
- 期：5
- 页码：1482 - 1486
- 全文大小：110K
- 年卷期：v.51,no.5(March 13, 2008)
- ISSN：1520-4804
文摘
Cocaine’s toxicity can be mitigated by blocking its interaction with sigma-1 receptors. The involvement of sigma-2 receptors remains unclear. To investigate their potential role, we have designed compounds through a convergent synthesis utilizing a highly selective sigma-1 ligand and elements of a selective sigma-2 ligand. Among the synthesized compounds was produced a subnanomolar sigma-2 ligand with an 11-fold preference over sigma-1 receptors. These compounds may be useful in developing effective pharmacotherapies for cocaine toxicity.