6-Alkoxyisoindolin-1-one based dopamine D 2 partial agonists as potential antipsychotics

A series of 6-alkoxyisoindolin-1-ones are presented as potential antipsychotics. The in vitro pharmacological profile includes D 2 partial agonism (30–55%), 5-HT 1A partial agonism (60–90%), and 5-HT 2A antagonism. Selected compounds in this series displayed good in vivo activity and potency. A seri...

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Published inBioorganic & medicinal chemistry letters Vol. 20; no. 19; pp. 5666 - 5669
Main Authors Favor, David A., Powers, James J., White, Andrew D., Fitzgerald, Lawrence W., Groppi, Vincent, Serpa, Kevin A.
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 01.10.2010
Subjects
Antipsychotics
Dopamine Partial agonist
Antipsychotics
Dopamine Partial agonist
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Summary:A series of 6-alkoxyisoindolin-1-ones are presented as potential antipsychotics. The in vitro pharmacological profile includes D 2 partial agonism (30–55%), 5-HT 1A partial agonism (60–90%), and 5-HT 2A antagonism. Selected compounds in this series displayed good in vivo activity and potency. A series of 6-alkoxyisoindolin-1-ones with a magic shotgun pharmacological profile are presented as potential antipsychotics. The in vitro pharmacological profile includes D 2 partial agonism (30–55%), 5-HT 1A partial agonism (60–90%), and 5-HT 2A antagonism. Selected compounds in this series displayed good in vivo activity and potency.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.08.023