Figure 1. CP55940-induced concentration-dependent stimulation of intracellular calcium mobilization in CHO-K1/CNR1/Gα15 cells. The cells were loaded with Calcium-4 prior to being stimulated with agonist, CP55940. 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 CP55940 (Mean ± SD, n = 2). The EC50 of CP55940 on this cell was 28.1 μM.
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/CB1/Gα15 Stable Cell Line
The cannabinoid receptor CNR1 is Gs-coupled GPCRs expressed in primarily CNS and some peripheral neurones; particularly prevalent in basal ganglia, hippocampus, cerebellum, cerebral cortex and also presented in some non-neuronal cells and tissues, for example leukocytes and testis. A shorter human splice variant (411aa) has been identified in the brain and other tissues by reverse-transcriptase PCR but mRNA levels were less than 10-fold the levels of the longer isoform. The pharmacological characteristics of the isoforms are similar.
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