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

Yinfa Yan, Ping Zhou, David 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 journalArticleResearchpeer-review

11 Citations (Scopus)

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

Fingerprint

Serotonin Uptake Inhibitors
Dopamine
Schizophrenia
Amines
Ligands
In Vitro Techniques

Keywords

  • Dopamine D partial agonist
  • Schizophrenia
  • Serotonin reuptake inhibitor

Cite this

Yan, Yinfa ; Zhou, Ping ; Rotella, David ; Feenstra, Rolf ; Kruse, Chris G. ; Reinders, Jan Hendrik ; Neut, Martina van der ; Lai, Margaret ; Zhang, Jean ; Kowal, Dianne M. ; Carrick, Tikva ; Marquis, Karen L. ; Pausch, Mark H. ; Robichaud, Albert J. / Potent dihydroquinolinone dopamine D2 partial agonist/serotonin reuptake inhibitors for the treatment of schizophrenia. In: Bioorganic and Medicinal Chemistry Letters. 2010 ; Vol. 20, No. 9. pp. 2983-2986.
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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.",
keywords = "Dopamine D partial agonist, Schizophrenia, Serotonin reuptake inhibitor",
author = "Yinfa Yan and Ping Zhou and David Rotella and Rolf Feenstra and Kruse, {Chris G.} and Reinders, {Jan Hendrik} and Neut, {Martina van der} and Margaret Lai and Jean Zhang and Kowal, {Dianne M.} and Tikva Carrick and Marquis, {Karen L.} and Pausch, {Mark H.} and Robichaud, {Albert J.}",
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Yan, Y, Zhou, P, Rotella, D, Feenstra, R, Kruse, CG, Reinders, JH, Neut, MVD, Lai, M, Zhang, J, Kowal, DM, Carrick, T, Marquis, KL, Pausch, MH & Robichaud, AJ 2010, 'Potent dihydroquinolinone dopamine D2 partial agonist/serotonin reuptake inhibitors for the treatment of schizophrenia', Bioorganic and Medicinal Chemistry Letters, vol. 20, no. 9, pp. 2983-2986. https://doi.org/10.1016/j.bmcl.2010.02.105

Potent dihydroquinolinone dopamine D2 partial agonist/serotonin reuptake inhibitors for the treatment of schizophrenia. / Yan, Yinfa; Zhou, Ping; Rotella, David; Feenstra, Rolf; Kruse, Chris G.; Reinders, Jan Hendrik; Neut, Martina van der; Lai, Margaret; Zhang, Jean; Kowal, Dianne M.; Carrick, Tikva; Marquis, Karen L.; Pausch, Mark H.; Robichaud, Albert J.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 20, No. 9, 01.05.2010, p. 2983-2986.

Research output: Contribution to journalArticleResearchpeer-review

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AU - Yan, Yinfa

AU - Zhou, Ping

AU - Rotella, David

AU - Feenstra, Rolf

AU - Kruse, Chris G.

AU - Reinders, Jan Hendrik

AU - Neut, Martina van der

AU - Lai, Margaret

AU - Zhang, Jean

AU - Kowal, Dianne M.

AU - Carrick, Tikva

AU - Marquis, Karen L.

AU - Pausch, Mark H.

AU - Robichaud, Albert J.

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