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Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid affinity
Authors:Roy Caroline  Li Ticheao  Krasik Pavel  Gilbert Marie-Joseé  Pelletier Christine  Gagnon Diane  Robert Ed  Ducharme Julie  Storer Richard  Lavallée Jean-François
Institution:Shire Biochem, 275 Armand-Frappier Blvd., Laval, H7V 4A7, Québec, Canada. croy@ca.shire.com
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.
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