Figure 1: Epinephrine-induced concentration-dependent stimulation of intracellular calcium mobilization in CHOK1/ADRA1A cells. The cells were loaded with Calcium-4 prior to being stimulated with an ADRA1A receptor agonist, epinephrine. The intracellular calcium change was measured by FLIPR. The relative fluorescent units (RFU) were plotted against the log of the cumulative doses (10-fold dilution) of epinephrine (Mean ± SD, n = 2). The EC50 of epinephrine on this cell was 0.72 nM.
Note:
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/ADRA1A Stable Cell Line
The α1-adrenergic receptor (AR) family consists of three closely related gene products (α1A, α1B, and α1D) that mediate the actions of norepinephrine (NE) and epinephrine in sympathetically innervated tissues and brain. α1-ARs belong to the G protein-coupled receptor family and consist of single polypeptide chains predicted to have seven transmembrane spanning domains. With similar pharmacological and signaling properties, α1-AR subtypes act through Gq/11 proteins to activate phospholipase C, increase both inositol 1,4,5-trisphosphate production and intracellular Ca2+. Once activated by binding, α1-ARs initiate the cellular pathways leading to the regulation of physiological effects, including blood pressure maintenance, glucose metabolism, renal sodium reabsorption, and cardiac inotropy.
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| 联系凯发一触即发 | |
