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Identification of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the management of cough and anxiety |
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| Authors: | Shu-Wei Yang Ginny Ho Deen Tulshian William J. Greenlee Zheng Tan Hongtao Zhang April Smith-Torhan Ahmad Fawzi John Anthes Sherry Lu Geoffrey Varty Xiomara Fernandez Robbie L. McLeod John Hey |
| Affiliation: | 1. Department of Chemical Research—CV & CNS, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA;2. Neurobiology Department of Biological Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA |
| Abstract: | A series of nortropane analogs based on previously reported compound 1 have been synthesized and shown to bind to the nociceptin receptor with high affinity. The synthesis and structure–activity relationships around the C-3 nortropane substitution are described. From the SAR study and hPXR screening effort, compound 15 was identified to possess potent oral antitussive and anxiolytic-like activities in the guinea pig models. |
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