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

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Yan Y, Zhou P, Rotella DP, Feenstra R, Kruse CG, Reinders JH, van der Neut M, Lai M, Zhang J, Kowal DM, Carrick T, Marquis KL, Pausch MH, Robichaud AJ

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

Bioorg Med Chem Lett. 2010 May 1;20(9):2983-6. doi: 10.1016/j.bmcl.2010.02.105. Epub 2010 Mar 3.

PubMed ID

20347298 [ View in PubMed

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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 D(2) ligands to prepare a series of dual acting compounds with attractive in vitro profiles as dopamine D(2) partial agonists and serotonin reuptake inhibitors. Structure-activity studies revealed that the linker plays a key role in contributing to D(2) affinity, function, and SRI activity.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Escitalopram	Sodium-dependent serotonin transporter	Ki (nM)	1	N/A	N/A	Details
Haloperidol	Dopamine D2 receptor	Ki (nM)	3	N/A	N/A	Details