Design, synthesis, and SAR analysis of novel selective σ1 ligands

Autor: Caterina Zanette, Mariangela Urbano, Alice Pedrali, Christian Laggner, Maria Grazia Mamolo, Bernard Wuensch, Massimo Serra, Ornella Azzolina, Daniele Zampieri, Simona Collina, Dirk Schepmann, Daniela Rossi, Chiara Florio
Rok vydání: 2007
Předmět:
Zdroj: Bioorganic & Medicinal Chemistry. 15:771-783
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2006.10.048
Popis: A new series of arylalkyl- and alkenylamines was designed, synthesized, and evaluated for binding to sigma(1) and sigma(2) receptors. Many compounds exhibited nanomolar affinity for sigma(1) subtype receptor with good selectivity over sigma(2). A molecular modeling study was conducted in order to rationalize the experimental data, and the structure-receptor affinities are discussed.
Databáze: OpenAIRE