Figure 1: Bradykinin-induced concentration-dependent stimulation of intracellular calcium mobilization in CHO-K1/B2/Gα15 cells. The cells were loaded with Calcium-4 prior to stimulation with a B2 receptor agonist, bradykinin. The intracellular calcium change was measured by FLIPR. The relative fluorescent units (RFU) were normalized and plotted against the log of the cumulative doses of bradykinin (Mean ± SD, n = 2). The EC50 value of bradykinin on this cell was 45.58 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 and starts at Bottom and goes to Top with a sigmoid shape.
CHO-K1/B2/Gα15 Stable Cell Line
Bradykinin (BK) is a pro-inflammatory polypeptide that can cause pain, inflammation, increased vascular permeability, vasodilation, contraction of various smooth muscles, and cell proliferation by stimulating B1and B2 receptors. B2 receptors are most commonly distributed in the vascular and non-vascular smooth muscle and in the heart. The B2 receptor mediates the action of bradykinin (BK) and lysyl-bradykinin (Lys-BK). The stimulation of BK B2 receptors is not only implicated in the pathogenesis of inflammation, pain, and tissue injury but also in cardioprotective mechanisms. So B2 receptor agonists may have important clinical value in the treatment and prevention of various cardiovascular disorders such as hypertension, ischaemic heart disease, left ventricular hypertrophy, ventricular remodeling, congestive heart failure, and diabetic disorders.
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