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Design, synthesis and SAR analysis of novel selective sigma(1) ligands (Part 2).

Bioorganic & medicinal chemistry 2009 Dec 21; In press

Link to PubMed abstract

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

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

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 mu-opioid, delta-opioid and kappa-opioid receptors. Biological results are herein presented and discussed.

Keywords: sigma1