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2 results on '"Jean, Zhang"'

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

Author

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

Subjects
Serotonin reuptake inhibitor, Clinical Biochemistry, Pharmaceutical Science, Pharmacology, Quinolones, Biochemistry, Partial agonist, Reuptake, Structure-Activity Relationship, Dopamine receptor D2, Drug Discovery, Moiety, Animals, Molecular Biology, biology, Chemistry, Receptors, Dopamine D2, Organic Chemistry, Disease Models, Animal, Norepinephrine transporter, Dopamine Agonists, Receptor, Serotonin, 5-HT1A, biology.protein, Schizophrenia, Molecular Medicine, Pharmacophore, Endogenous agonist, Selective Serotonin Reuptake Inhibitors, Antipsychotic Agents
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.

Published
2010

2. Tetrahydrocarbazole-based serotonin reuptake inhibitor/dopamine D2 partial agonists for the potential treatment of schizophrenia

Author

Jean Zhang, Julie A. Brennan, Chris G. Kruse, Jan-Hendrik Reinders, Dianne Kowal, Geraldine Ruth Mcfarlane, Feenstra Roelof W, Sara Núñez-García, Andrew C. McCreary, Karen L. Marquis, Radka Graf, Mark H. Pausch, Alexander Greenfield, Margaret Lai, Albert J. Robichaud, Farhana Pruthi, Tikva Carrick, David P. Rotella, Cristina Grosanu, Steven M. Grauer, Rajiah A. Denny, Kelly Sullivan, Rachel Navarra, and Martina A.W. van der Neut

Subjects
medicine.medical_treatment, Serotonin reuptake inhibitor, Clinical Biochemistry, Carbazoles, Pharmaceutical Science, Pharmacology, Serotonin 5-HT1 Receptor Antagonists, Biochemistry, Partial agonist, chemistry.chemical_compound, In vivo, Dopamine receptor D2, Drug Discovery, medicine, Animals, Antipsychotic, Neurotransmitter, Molecular Biology, Receptors, Dopamine D2, Organic Chemistry, Rats, Disease Models, Animal, chemistry, Dopamine Agonists, Receptor, Serotonin, 5-HT1A, Schizophrenia, Molecular Medicine, Serotonin, Reuptake inhibitor, Selective Serotonin Reuptake Inhibitors
Abstract

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.

Published
2009

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