Tetrahydrocarbazole-based serotonin reuptake inhibitor/dopamine D 2 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 D 2 receptor ligands in an attempt to identify potent D 2 partial agonist/SRI molecules for treatment of schizophrenia. This approach has the potential to treat a broa...

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Published inBioorganic & medicinal chemistry letters Vol. 19; no. 19; pp. 5552 - 5555
Main Authors Rotella, David P., 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., Pausch, Mark H.
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 01.10.2009
Subjects
Dopamine D 2 partial agonist
Dual-acting molecule
Schizophrenia
SRI
Schizophrenia
SRI
Dual-acting molecule
Dopamine D 2 partial agonist
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Summary:A 5-fluoro-tetrahydrocarbazole serotonin reuptake inhibitor (SRI) building block was combined with a variety of linkers and dopamine D 2 receptor ligands in an attempt to identify potent D 2 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 D 2 partial agonism in cell-based and in vivo assays.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.08.050