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Design,synthesis and SAR analysis of novel selective σ1 ligands (Part 2)
Authors:Daniela Rossi  Mariangela Urbano  Alice Pedrali  Massimo Serra  Daniele Zampieri  Maria Grazia Mamolo  Christian Laggner  Caterina Zanette  Chiara Florio  Dirk Schepmann  Bernard Wuensch  Ornella Azzolina  Simona Collina
Institution:1. Department of Pharmaceutical Chemistry, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy;2. Department of Pharmaceutical Sciences, University of Trieste, P.le Europa 1, 34127 Trieste, Italy;3. Institute of Pharmacy, Department of Pharmaceutical Chemistry and Center for Molecular Biosciences Innsbruck (CMBI), University of Innsbruck, Innrain 52c, 6020 Innsbruck, Austria;4. Department of Biomedical Sciences (Pharmacology Section), University of Trieste, Via Giorgieri 7, 34127 Trieste, Italy;5. Institute of Pharmaceutical and Medicinal Chemistry, University of Muenster, Hittorfstrasse 58-62, 48149 Muenster, Germany
Abstract:In order to investigate the molecular features involved in sigma receptors (σ-Rs) binding, new compounds based on arylalkylaminoalcoholic, arylalkenyl- and arylalkylaminic scaffolds were synthesized and their affinity towards σ1- and σ2-Rs subtypes was evaluated. The most promising compounds were also screened for their affinity at μ-opioid, δ-opioid and κ-opioid receptors. Biological results are herein presented and discussed.
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