Potent Dihydroquinolinone Dopamine D2 Partial Agonist/Serotonin Reuptake Inhibitors for the Treatment of Schizophrenia
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.
MSU Digital Commons Citation
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.; and Robichaud, Albert J., "Potent Dihydroquinolinone Dopamine D2 Partial Agonist/Serotonin Reuptake Inhibitors for the Treatment of Schizophrenia" (2010). Department of Chemistry and Biochemistry Faculty Scholarship and Creative Works. 23.