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J Med Chem. 2008 Mar 13;51(5):1482-6. doi: 10.1021/jm701357m. Epub 2008 Feb 16.

Conversion of a highly selective sigma-1 receptor-ligand to sigma-2 receptor preferring ligands with anticocaine activity.

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Department of Medicinal Chemistry, The University of Mississippi, Mississippi 38677, USA.


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.

[Indexed for MEDLINE]

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