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In vitro functional bioassays at cells transfected with human 5HT2A receptor (aequorin and luminescence-based intracellular calcium assay)
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Tested and reference compounds were dissolved in DMSO at a concentration of 10–2 M. Serial dilutions were prepared in 96-well microplate in assay buffer and eight to ten concentrations were tested.
A cellular aequorin-based functional assay was performed with recombinant Chinese hamster ovary cells expressing mitochondrially targeted aequorin, human G-protein-coupled receptors, and the promiscuous G protein α16 for 5-HT2A. The full description of this assay is in Supplementary materials.
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