Design, synthesis, and SAR analysis of novel selective sigma1 ligands

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 ra...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2007-01, Vol.15 (2), p.771-783
Hauptverfasser:	Collina, Simona, Loddo, Guya, Urbano, Mariangela, Linati, Laura, Callegari, Athos, Ortuso, Francesco, Alcaro, Stefano, Laggner, Christian, Langer, Thierry, Prezzavento, Orazio, Ronsisvalle, Giuseppe, Azzolina, Ornella
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Brain - metabolism Chemical Phenomena Chemistry, Physical Chromatography, Thin Layer Drug Design Guinea Pigs In Vitro Techniques Indicators and Reagents Magnetic Resonance Spectroscopy Membranes - metabolism Models, Molecular Molecular Conformation Radioligand Assay Receptors, sigma - drug effects Sigma-1 Receptor Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0968-0896