Synthesis and pharmacological evaluation of indole-based sigma receptor ligands
(2011) European Journal of Medicinal Chemistry — Vol. 46, n° 10, p. 5154-5161 (2011)
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- A series of novel indole-based analogs were prepared and their affinities for sigma receptors were determined using in vitro radioligand binding assays. The results of this study identified several compounds with nanomolar sigma-2 affinity and significant selectivity over sigma-1 receptors. In particular, 2-(4-(3-(4-fluorophenyl)indol-1-yl)butyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline (9f) was found to display high affinity at sigma-2 receptors with good selectivity (σ-1/σ-2 = 395). The pharmacological binding profile for this compound was established with other relevant non-sigma sites.
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Mésangeau, C., Amata, E., Alsharif, W., Seminerio, M. J., Robson, M. J., Matsumoto, R. R., Poupaert, J., & McCurdy, C. R. (2011). Synthesis and pharmacological evaluation of indole-based sigma receptor ligands. European Journal of Medicinal Chemistry, 46(10), 5154-5161. https://doi.org/10.1016/j.ejmech.2011.08.031 (Original work published 2011)