The calcium influx assay is the most robust and suitable first-line high-throughput screening method for discovering P2X7 receptor ligands.
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Calcium influx assay offers superior robustness for P2X7R ligand screening; extends in vitro methodology but leaves open in vivo translation.
The P2X 7 receptor (P2X 7 R) is an important member of the P2X family of ligand-gated ion channels that respond to ATP as the endogenous agonist. Studies suggest that P2X 7 R plays a potentially pivotal role in a variety of physiological functions, including peripheral and central neuronal transmission, smooth muscle contraction, and inflammation. Thus, P2X 7 R may be a potential target for drug development. Here, we used a FlexStation to examine the function of recombinant P2X 7 R stably expressed in human embryonic kidney 293 cells and to compare three high-throughput screening assays: a membrane potential assay, an ethidium bromide uptake assay, and a calcium influx assay. We found that all three assays were suitable for the analysis of P2X 7 R, but the calcium influx assay was the most robust and is the best choice as a first high-throughput screening assay when embarking on a P2X 7 R drug discovery project.
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Jiang et al. (2013) studied this question.
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