title: Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid affinity.
abstract: Several novel racemic aminotetralin derivatives have been prepared using a stereoselective aziridine ring opening reactions and were evaluated for their micro-opioid receptor binding affinity. Selectivity index towards other opioid receptors and antinociceptive activity in mice have been evaluated for the most potent derivatives.
authors.affiliation: Shire Biochem, 275 Armand-Frappier Blvd., Laval, H7V 4A7, Québec, Canada. croy@ca.shire.com
authors.forename: Caroline
authors.initials: C
authors.lastname: Roy
authors.forename: Ticheao
authors.initials: T
authors.lastname: Li
authors.forename: Pavel
authors.initials: P
authors.lastname: Krasik
authors.forename: Marie-Joseé
authors.initials: MJ
authors.lastname: Gilbert
authors.forename: Christine
authors.initials: C
authors.lastname: Pelletier
authors.forename: Diane
authors.initials: D
authors.lastname: Gagnon
authors.forename: Ed
authors.initials: E
authors.lastname: Robert
authors.forename: Julie
authors.initials: J
authors.lastname: Ducharme
authors.forename: Richard
authors.initials: R
authors.lastname: Storer
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Lavallée
mesh_terms: D000701:Analgesics, Opioid / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D007202:Indicators and Reagents; D051379:Mice; D010147:Pain Measurement / Q000187:drug effects; D017465:Receptors, Opioid, delta / Q000187:drug effects / Q000378:metabolism; D017473:Receptors, Opioid, kappa / Q000187:drug effects / Q000378:metabolism; D017450:Receptors, Opioid, mu / Q000187:drug effects*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000701:Analgesics, Opioid; D007202:Indicators and Reagents; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D013764:Tetrahydronaphthalenes