Figure 1. 5-HT-induced concentration-dependent stimulation of intracellular calcium mobilization in CHO-K1/5-HT2A cells. The cells were loaded with Calcium-4 prior to being stimulated with a 5-HT2A receptor agonist, 5-HT. The intracellular calcium change was measured by FLIPRTETRA. The relative fluorescent units (RFU) were normalized and plotted against the log of the cumulative doses (5-fold dilution) of 5-HT (Mean ± SD, n = 2). The EC50 of 5-HT on this cell was 10.2 nM.
Notes:
1. EC50 value is calculated with four parameter logistic equation:
Y=Bottom + (Top-Bottom)/(1+10^((LogEC50-X)*HillSlope))
X is the logarithm of concentration. Y is the response
Y is RFU and starts at Bottom and goes to Top with a sigmoid shape.
CHO-K1/5-HT2A Stable Cell Line
5-Hydroxytryptamine (5-HT, also commonly known as serotonin) is synthesized in enterochromaffin cells in the intestine and in serotonergic nerve terminals. In the periphery, 5-HT mediates gastrointestinal motility, platelet aggregation, and contraction of blood vessels. Many functions of the central nervous system are influenced by 5-HT, including sleep, motor activity, sensory perception, arousal, and appetite. A family of 12 GPCRs and one ion channel mediate the biological effects of 5-HT (Hoyer et al., 1994). 5-HT2A which couples to Gq/11 is expressed throughout the central nervous system in the neocortex and olfactory tubercle. 5-HT2A receptor agonists may have important clinical value in the treatment of various disorders, such as depression, anxiety, bipolar disorder, and schizophrenia. GenScript's cloned human 5-HT2A–expressing cell line is generated in the CHO-K1 host.
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