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. 2022 Mar 14;16:826289. doi: 10.3389/fnins.2022.826289

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Copyright © 2022 Kirchweger, Klein-Junior, Pretsch, Chen, Cretton, Gasper, Heyden, Christen, Kirchmair, Henriques and Rollinger.

This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

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(A) Nemorosine A (1) aligned with 6-methoxy-N,N-dimethyl-1,3,4,5-tetrahydrobenzo[cd]indol-4-amine (ChEMBL49309), a known antagonist of the 5-HT₁ and 5-HT₂ receptors. (B) 5-HT competitive inhibition of 5HT_2A by 1 and 2 at different concentrations in HEK-293T cells. Data were normalized to the positive control wells (ketanserin), which were expressed as 100% inhibition. Bars represent the mean inhibition of two independent experiments ± SD. (C) Concentration-dependent increase in 5HT_2A activity in HEK-293T cells in response to 1 and 2. Bars represent the mean of two independent experiments ± SD. Vehicle control was set to 0% inhibition. Significance was evaluated with one-way ANOVA–Bonferoni post hoc test (***p < 0.001 vs. vehicle control).