[Establishment and application of a high-throughput screening method for drugs targeting the 5-hydroxytryptamine 2A receptor based on cellular calcium flux signals].
Sheng wu gong cheng xue bao = Chinese journal of biotechnology August 25, 2025 Bingqian Zhang, Jingjing Shi, Yi Zhang et al.
A high-throughput screening method for drugs targeting the 5-HT2A receptor was developed using calcium flux signals. The method, optimized with 10,000 cells per well, 0.2% DMSO, and 2-hour Calcium 6 dye incubation, showed excellent specificity and precision (inter-batch precision below 10% for 5-HT detection). Testing four known compounds (DOI, 5-MeO-DMT, LSD, and MDL100907) yielded Z'-factors above 0.85 and signal window values over 0.91 at EC80, with EC50 values in the nanomolar range. Applied to 38 known active compounds, it efficiently identified agonists and antagonists without responding to non-target compounds, confirming its reliability for screening antidepressants targeting the 5-HT2A receptor.