Conversion of a highly selective sigma-1 receptor-ligand to sigma-2 receptor preferring ligands with anticocaine activity
(2008) Journal of Medicinal Chemistry — Vol. 51, n° 5, p. 1482-1486 (2008)
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- Abstract
- 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.
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Mésangeau, C., Narayanan, S., Green, A. M., Shaikh, J., Kaushal, N., Viard, E., Xu, Y.-T., Fishback, J. A., Poupaert, J., Matsumoto, R. R., & McCurdy, C. R. (2008). Conversion of a highly selective sigma-1 receptor-ligand to sigma-2 receptor preferring ligands with anticocaine activity. Journal of Medicinal Chemistry, 51(5), 1482-1486. https://doi.org/10.1021/jm701357m (Original work published 2008)