Bioorganic and Medicinal Chemistry Letters p. 5552 - 5555 (2009)
Update date:2022-08-10
Topics:
Rotella, David P.
McFarlane, Geraldine R.
Greenfield, Alexander
Grosanu, Cristina
Robichaud, Albert J.
Denny, Rajiah Aldrin
Feenstra, Rolf W.
Nunez-Garcia, 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.
Pausch, Mark H.
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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