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Tetrahydrocarbazole-based serotonin reuptake inhibitor/dopamine D2 partial agonists for the potential treatment of schizophrenia |
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| Authors: | David P. Rotella Geraldine R. McFarlane Alexander Greenfield Cristina Grosanu Albert J. Robichaud Rajiah Aldrin Denny Rolf W. Feenstra Sara Núñez-García Jan-Hendrik Reinders Martina van der Neut Andrew McCreary Chris G. Kruse Kelly Sullivan Farhana Pruthi Margaret Lai Jean Zhang Dianne M. Kowal Tikva Carrick Steven M. Grauer Rachel L. Navarra Mark H. Pausch |
| Affiliation: | 1. Chemical Sciences, Wyeth Research, CN 8000 Princeton, NJ 08543, United States;2. Solvay Pharmaceuticals Research Laboratories, C.J. van Houtenlaan 36, 1381 CP Weesp, The Netherlands;3. Discovery Neuroscience, Wyeth Research, CN 8000 Princeton, NJ 08543, United States |
| Abstract: | A 5-fluoro-tetrahydrocarbazole serotonin reuptake inhibitor (SRI) building block was combined with a variety of linkers and dopamine D2 receptor ligands in an attempt to identify potent D2 partial agonist/SRI molecules for treatment of schizophrenia. This approach has the potential to treat a broader range of symptoms compared to existing therapies. Selected compounds in this series demonstrate high affinity for both targets and D2 partial agonism in cell-based and in vivo assays. |
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