title: Design, synthesis and SAR analysis of novel selective sigma1 ligands (Part 2).
abstract: 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 micro-opioid, delta-opioid and kappa-opioid receptors. Biological results are herein presented and discussed.
authors.affiliation: Department of Pharmaceutical Chemistry, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy.
authors.forename: Daniela
authors.initials: D
authors.lastname: Rossi
authors.forename: Mariangela
authors.initials: M
authors.lastname: Urbano
authors.forename: Alice
authors.initials: A
authors.lastname: Pedrali
authors.forename: Massimo
authors.initials: M
authors.lastname: Serra
authors.forename: Daniele
authors.initials: D
authors.lastname: Zampieri
authors.forename: Maria Grazia
authors.initials: MG
authors.lastname: Mamolo
authors.forename: Christian
authors.initials: C
authors.lastname: Laggner
authors.forename: Caterina
authors.initials: C
authors.lastname: Zanette
authors.forename: Chiara
authors.initials: C
authors.lastname: Florio
authors.forename: Dirk
authors.initials: D
authors.lastname: Schepmann
authors.forename: Bernard
authors.initials: B
authors.lastname: Wuensch
authors.forename: Ornella
authors.initials: O
authors.lastname: Azzolina
authors.forename: Simona
authors.initials: S
authors.lastname: Collina
mesh_terms: D000475:Alkenes / Q000737:chemistry / Q000494:pharmacology; D000588:Amines / Q000737:chemistry* / Q000494:pharmacology*; D000605:Amino Alcohols / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D006168:Guinea Pigs; D006841:Hydrocarbons, Aromatic / Q000737:chemistry / Q000494:pharmacology; D008024:Ligands; D008958:Models, Molecular; D011485:Protein Binding; D051381:Rats; D011957:Receptors, Opioid / Q000378:metabolism; D017480:Receptors, sigma / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D000475:Alkenes; D000588:Amines; D000605:Amino Alcohols; D006841:Hydrocarbons, Aromatic; D008024:Ligands; D011957:Receptors, Opioid; D017480:Receptors, sigma