Bioorg Med Chem. 2010 Feb;18(3):1204-12. Epub 2009 Dec 21.

Design, synthesis and SAR analysis of novel selective sigma1 ligands (Part 2).

Rossi D, Urbano M, Pedrali A, Serra M, Zampieri D, Mamolo MG, Laggner C, Zanette C, Florio C, Schepmann D, Wuensch B, Azzolina O, Collina S.

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Department of Pharmaceutical Chemistry, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy.

Abstract

In order to investigate the molecular features involved in sigma receptors (sigma-Rs) binding, new compounds based on arylalkylaminoalcoholic, arylalkenyl- and arylalkylaminic scaffolds were synthesized and their affinity towards sigma(1)- and sigma(2)-Rs subtypes was evaluated. The most promising compounds were also screened for their affinity at micro-opioid, delta-opioid and kappa-opioid receptors. Biological results are herein presented and discussed.

PMID:: 20045339; [PubMed - indexed for MEDLINE]

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