Tetrahydrocarbazole-Based Serotonin Reuptake Inhibitor/Dopamine D2 Partial Agonists for the Potential Treatment of Schizophrenia
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.
MSU Digital Commons Citation
Rotella, David; McFarlane, Geraldine R.; Greenfield, Alexander; Grosanu, Cristina; Robichaud, Albert J.; Denny, Rajiah Aldrin; Feenstra, Rolf W.; Núñez-García, Sara; Reinders, Jan Hendrik; Neut, Martina van der; McCreary, Andrew; Kruse, Chris G.; Sullivan, Kelly; Pruthi, Farhana; Lai, Margaret; Zhang, Jean; Kowal, Dianne M.; Carrick, Tikva; Grauer, Steven M.; Navarra, Rachel L.; Graf, Radka; Brennan, Julie; Marquis, Karen L.; and Pausch, Mark H., "Tetrahydrocarbazole-Based Serotonin Reuptake Inhibitor/Dopamine D2 Partial Agonists for the Potential Treatment of Schizophrenia" (2009). Department of Chemistry and Biochemistry Faculty Scholarship and Creative Works. 20.