Matthew Robson
Research Fellow
Last active: 10/19/2015

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

Mésangeau C, Amata E, Alsharif W, Seminerio MJ, Robson MJ, Matsumoto RR, Poupaert JH, McCurdy CR
Eur J Med Chem. 2011 46 (10): 5154-61

PMID: 21899931 · PMCID: PMC3272488 · DOI:10.1016/j.ejmech.2011.08.031

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.

Copyright © 2011. Published by Elsevier Masson SAS.

MeSH Terms (10)

Animals Cell Line Humans Indoles Ligands Protein Binding Radioligand Assay Rats Receptors, sigma Structure-Activity Relationship

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