Figure 1. CCK-8-induced concentration-dependent stimulation of intracellular calcium mobilization in CHO-K1/Gα15/CCKA cells. The cells were loaded with Calcium-4 prior to stimulation with a CCKA receptor agonist, CCK-8. The intracellular calcium change was measured by FLIPR. The relative fluorescent units (RFU) were plotted against the log of the cumulative doses of CCK-8 (Mean ± SD, n = 2). The EC50 of CCK-8 on this cell was 0.45 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.
2. Signal to background Ratio (S/B) = Top/Bottom
CHO-K1/CCKA/Gα15 Stable Cell Line
Cholecystokinin (CCK)-A and CCK-B receptors are highly homologous members of the seven transmembrane domain G-protein-coupled receptor super-family. Peptides in the cholecystokinin (CCK) family have a variety of biological functions in the central and peripheral nervous systems as well as in the gastrointestinal tract. The CCKA receptor has a more limited distribution with the highest densities in the hypothalamic nuclei, areas of the hippocampus, the septum, dorsal motor vagal nucleus, and interpeduncular nucleus of the brain stem. It also occurs in numerous gastro-intestinal tissues. Binding of ligands to CCK1 stimulates mobilization of intracellular calcium by activation of Gq/11. CCKA receptors affect satiety, pancreatitis, and gut motility and have growth-promoting effects on some tumors.
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