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-tetrahydroisoquin oline (9f) was found to display high affinity at sigma-2 receptors with good selectivity (sigma-1/sigma-2 = 395). The pharmacological binding profile for this compound was established with other relevant non-sigma sites.
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