title: Design, synthesis, and SAR analysis of novel selective sigma1 ligands.
abstract: 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.
authors.affiliation: Dipartimento di Chimica Farmaceutica, Università di Pavia, Viale Taramelli 12, 27100 Pavia, Italy. simona.collina@unipv.it
authors.forename: Simona
authors.initials: S
authors.lastname: Collina
authors.forename: Guya
authors.initials: G
authors.lastname: Loddo
authors.forename: Mariangela
authors.initials: M
authors.lastname: Urbano
authors.forename: Laura
authors.initials: L
authors.lastname: Linati
authors.forename: Athos
authors.initials: A
authors.lastname: Callegari
authors.forename: Francesco
authors.initials: F
authors.lastname: Ortuso
authors.forename: Stefano
authors.initials: S
authors.lastname: Alcaro
authors.forename: Christian
authors.initials: C
authors.lastname: Laggner
authors.forename: Thierry
authors.initials: T
authors.lastname: Langer
authors.forename: Orazio
authors.initials: O
authors.lastname: Prezzavento
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Ronsisvalle
authors.forename: Ornella
authors.initials: O
authors.lastname: Azzolina
mesh_terms: D000818:Animals; D001921:Brain / Q000378:metabolism; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002855:Chromatography, Thin Layer; D015195:Drug Design; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008566:Membranes / Q000378:metabolism; D008958:Models, Molecular; D008968:Molecular Conformation; D011869:Radioligand Assay; D017480:Receptors, sigma / Q000187:drug effects*; D013329:Structure-Activity Relationship; D000097605:Sigma-1 Receptor
chemical_list: D007202:Indicators and Reagents; D017480:Receptors, sigma; D000097605:Sigma-1 Receptor