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. 2019 Sep 16;13:3229–3248. doi: 10.2147/DDDT.S188760

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© 2019 Kiss et al.

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CAR and DDCAR are full agonists in cAMP accumulation assay in CHO cells expressing human serotonin 5-HT_1A receptors, whereas DCAR demonstrates partial agonist activity. cAMP levels were determined by the HTRF method given by the vendor (Cisbio).

Abbreviations: CAR, cariprazine; CHO, Chinese hamster ovary; DCAR, desmethyl-cariprazine; DDCAR, didesmethyl-cariprazine; E_max (%), percent maximal stimulation; FSK, forskolin; HTRF, homogeneous time-resolved fluorescence; pEC₅₀, negative logarithm of concentration of a drug that gives half-maximal response.