Potent dihydroquinolinone dopamine D2 partial agonist/serotonin reuptake inhibitors for the treatment of schizophrenia

Yinfa Yan, Ping Zhou, David P. Rotella, Rolf Feenstra, Chris G. Kruse, Jan Hendrik Reinders, Martina van der Neut, Margaret Lai, Jean Zhang, Dianne M. Kowal, Tikva Carrick, Karen L. Marquis, Mark H. Pausch, Albert J. Robichaud

Research output: Contribution to journalArticlepeer-review

12 Scopus citations

Abstract

A dihydroquinolinone moiety was found to be a potent serotonin reuptake inhibitor pharmacophore when combined with certain amines. This fragment was coupled with selected D2 ligands to prepare a series of dual acting compounds with attractive in vitro profiles as dopamine D2 partial agonists and serotonin reuptake inhibitors. Structure-activity studies revealed that the linker plays a key role in contributing to D2 affinity, function, and SRI activity.

Original languageEnglish
Pages (from-to)2983-2986
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number9
DOIs
StatePublished - 1 May 2010

Keywords

  • Dopamine D partial agonist
  • Schizophrenia
  • Serotonin reuptake inhibitor

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