کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1394579 | 1501172 | 2011 | 8 صفحه PDF | دانلود رایگان |
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.
A series of novel indole-based analogs were prepared and their affinities for sigma receptors were determined.Figure optionsDownload as PowerPoint slideHighlights
► Preparation and evaluation of a series of indoles as sigma receptor ligands.
► Identification of several sigma-2 selective derivatives.
► Extensive pharmacological profile characterization for the best compound.
Journal: European Journal of Medicinal Chemistry - Volume 46, Issue 10, October 2011, Pages 5154–5161