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. 2018 May 25;8:8137. doi: 10.1038/s41598-018-26401-9

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© The Author(s) 2018

Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.

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Multiplexed GPCR activity profiles induced by antipsychotic drugs. (a) Graphical representation of stimulation conditions in compound profiling GPCR assay monitoring effects of the antipsychotic drugs paliperidone and aripiprazole. GPCRs were stimulated with antipsychotic drugs alone to monitor receptor activating agonistic compound effects and in combination with agonist-mix to detect antagonistic receptor inhibiting compound effects. (b) Heatmap of agonistic compound effects. GPCRs were stimulated with paliperidone and aripiprazole at the indicated concentrations. (c) Heatmap of antagonistic compound effects. GPCRs were stimulated with drugs as indicated together with agonist-mix containing the agonists serotonin, dopamine, epinephrine, histamine, vasopressin and somatostatin each at 1 µM. Agonist-mix was added 1 h after drugs. Validation of drug induced effects by dose response curves of standard single luciferase GPCR split TEV assays of (d) receptor activation of the dopamine receptor DRD2 by aripiprazole, (e) receptor inhibition of the dopamine receptor DRD2 and (f) the serotonin receptor HTR2A by paliperidone.