Abstract
Calcium signaling plays a major role in the function of cells. Measurement of intracellular calcium mobilization is a robust assay that can be performed in a high-throughput manner to study the effect of compounds on potential drug targets. Pharmaceutical companies frequently use calcium signaling assays to screen compound libraries on G-protein-coupled receptors (GPCRs). In this chapter we describe the application of FLIPR technology to the evaluation of GPCR-induced calcium mobilization. We also include the implications of GPCR hetero-oligomerization and the identification of heteromeric receptors as novel drug targets on high-throughput calcium screening.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Benzylidene Compounds / pharmacology*
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Calcium Signaling
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Cell Culture Techniques
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Drug Evaluation, Preclinical / methods*
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Enkephalin, D-Penicillamine (2,5)- / pharmacology*
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HEK293 Cells
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High-Throughput Screening Assays / methods*
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Humans
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Naltrexone / analogs & derivatives*
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Naltrexone / pharmacology
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Receptors, G-Protein-Coupled / agonists
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Receptors, G-Protein-Coupled / antagonists & inhibitors
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Receptors, G-Protein-Coupled / biosynthesis
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Receptors, Opioid, delta / agonists*
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Receptors, Opioid, delta / antagonists & inhibitors
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Receptors, Opioid, delta / biosynthesis
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Recombinant Proteins / agonists
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Recombinant Proteins / antagonists & inhibitors
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Recombinant Proteins / biosynthesis
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Spectrometry, Fluorescence
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Transfection
Substances
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Benzylidene Compounds
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Receptors, G-Protein-Coupled
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Receptors, Opioid, delta
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Recombinant Proteins
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7-benzylidenenaltrexone
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Naltrexone
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Enkephalin, D-Penicillamine (2,5)-