Figure 1. U-50488-induced concentration-dependent stimulation of intracellular calcium mobilization in CHO-K1/OPRK1/Gα15 cells. The cells were loaded with Calcium-4 prior to being stimulated with agonist U-50488. The intracellular calcium change was measured by FLIPRTETRA. The relative fluorescent units (RFU) were normalized and plotted against the log of the cumulative doses of U-50488 (Mean ± SD, n = 2). The EC50 of U-50488 on this cell was 11 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/OPRK1/Gα15 Stable Cell Line
Opioid receptors and their endogenous peptide ligands play important roles in the reward and reinforcement of drugs such as heroin, cocaine, and alcohol. The κ-opioid receptor is a type of opioid receptor which binds the peptide opioid dynorphin as the primary endogenous ligand. κ-opioid receptors are widely distributed in the brain, spinal cord, and in pain neurons. They are associated with the risk for alcohol dependence.
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