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