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Eur J Med Chem. 2011 Oct;46(10):5154-61. doi: 10.1016/j.ejmech.2011.08.031. Epub 2011 Aug 29.

Synthesis and pharmacological evaluation of indole-based sigma receptor ligands.

Author information

1
Department of Medicinal Chemistry, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.

Abstract

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.

PMID:
21899931
PMCID:
PMC3272488
DOI:
10.1016/j.ejmech.2011.08.031
[Indexed for MEDLINE]
Free PMC Article

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